TY  - JOUR
AU  - Petrou, Anthi
AU  - Kartsev, Victor
AU  - Geronikaki, Athina
AU  - Glamočlija, Jasmina
AU  - Ćirić, Ana
AU  - Soković, Marina
PY  - 2023
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/5796
AB  - Nine new functionally substituted derivatives of 2-aminothiazole 
were evaluated for antimicrobial activity using microdilution 
method against the panel of eight bacterial and eight fungal strains. 
Evaluation of antibacterial activity revealed that compounds are 
potent antibacterial agents, more active than ampicillin and strep tomycin except of some compounds against B. cereus and En. 
cloacae. The best compound appeared to be compound 8. The 
most sensitive bacteria appeared to be En. cloacae, while L. mono cytogenes was the most resistant. Compounds also exhibited good 
antifungal activity much better than two reference drugs, ketoco nazole and bifonazole. Compound 1 exhibited the best antifungal 
activity. The most sensitive fungus was T. viride, while A. fumigatus 
was the most resistant. Bacteria as well as fungi in general showed 
different sensitivity towards compounds tested. Molecular docking 
studies revealed that MurB inhibition is probably involved in the 
mechanism of antibacterial activity, while CYP51 of C. albicans is 
responsible for the mechanism of antifungal activity. Finally, it 
should be mentioned that all compounds displayed very good 
druglikeness scores
PB  - Taylor & Francis Group
T2  - SAR and QSAR in Environmental Research
T1  - Functionally substituted 2-aminothiazoles as antimicrobial agents: in vitro and in silico evaluation
IS  - 5
VL  - 34
DO  - 10.1080/1062936X.2023.2214869
SP  - 359
EP  - 414
ER  - 

@article{
author = "Petrou, Anthi and Kartsev, Victor and Geronikaki, Athina and Glamočlija, Jasmina and Ćirić, Ana and Soković, Marina",
year = "2023",
abstract = "Nine new functionally substituted derivatives of 2-aminothiazole 
were evaluated for antimicrobial activity using microdilution 
method against the panel of eight bacterial and eight fungal strains. 
Evaluation of antibacterial activity revealed that compounds are 
potent antibacterial agents, more active than ampicillin and strep tomycin except of some compounds against B. cereus and En. 
cloacae. The best compound appeared to be compound 8. The 
most sensitive bacteria appeared to be En. cloacae, while L. mono cytogenes was the most resistant. Compounds also exhibited good 
antifungal activity much better than two reference drugs, ketoco nazole and bifonazole. Compound 1 exhibited the best antifungal 
activity. The most sensitive fungus was T. viride, while A. fumigatus 
was the most resistant. Bacteria as well as fungi in general showed 
different sensitivity towards compounds tested. Molecular docking 
studies revealed that MurB inhibition is probably involved in the 
mechanism of antibacterial activity, while CYP51 of C. albicans is 
responsible for the mechanism of antifungal activity. Finally, it 
should be mentioned that all compounds displayed very good 
druglikeness scores",
publisher = "Taylor & Francis Group",
journal = "SAR and QSAR in Environmental Research",
title = "Functionally substituted 2-aminothiazoles as antimicrobial agents: in vitro and in silico evaluation",
number = "5",
volume = "34",
doi = "10.1080/1062936X.2023.2214869",
pages = "359-414"
}

Petrou, A., Kartsev, V., Geronikaki, A., Glamočlija, J., Ćirić, A.,& Soković, M.. (2023). Functionally substituted 2-aminothiazoles as antimicrobial agents: in vitro and in silico evaluation. in SAR and QSAR in Environmental Research
Taylor & Francis Group., 34(5), 359-414.
https://doi.org/10.1080/1062936X.2023.2214869

Petrou A, Kartsev V, Geronikaki A, Glamočlija J, Ćirić A, Soković M. Functionally substituted 2-aminothiazoles as antimicrobial agents: in vitro and in silico evaluation. in SAR and QSAR in Environmental Research. 2023;34(5):359-414.
doi:10.1080/1062936X.2023.2214869 .

Petrou, Anthi, Kartsev, Victor, Geronikaki, Athina, Glamočlija, Jasmina, Ćirić, Ana, Soković, Marina, "Functionally substituted 2-aminothiazoles as antimicrobial agents: in vitro and in silico evaluation" in SAR and QSAR in Environmental Research, 34, no. 5 (2023):359-414,
https://doi.org/10.1080/1062936X.2023.2214869 . .

TY  - JOUR
AU  - Petrou, Anthi
AU  - Geronikaki, Athina
AU  - Kartsev, Victor
AU  - Kousaxidis, Antonios
AU  - Papadimitriou-Tsantarliotou, Aliki
AU  - Kostić, Marina
AU  - Ivanov, Marija
AU  - Soković, Marina
AU  - Nicolaou, Ioannis
AU  - Vizirianakis, Ioannis S.
PY  - 2023
UR  - https://www.mdpi.com/1424-8247/16/1/131
UR  - http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC9865890
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/5459
AB  - Herein, we report the experimental evaluation of the antimicrobial activity of seventeen new (Z)-methyl 3-(4-oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylate derivatives. All tested compounds exhibited antibacterial activity against eight Gram-positive and Gram-negative bacteria. Their activity exceeded those of ampicillin as well as streptomycin by 10-50 fold. The most sensitive bacterium was En. Cloacae, while E. coli was the most resistant one, followed by M. flavus. The most active compound appeared to be compound 8 with MIC at 0.004-0.03 mg/mL and MBC at 0.008-0.06 mg/mL. The antifungal activity of tested compounds was good to excellent with MIC in the range of 0.004-0.06 mg/mL, with compound 15 being the most potent. T. viride was the most sensitive fungal, while A. fumigatus was the most resistant one. Docking studies revealed that the inhibition of E. coli MurB is probably responsible for their antibacterial activity, while 14a-lanosterol demethylase of CYP51Ca is involved in the mechanism of antifungal activity. Furthermore, drug-likeness and ADMET profile prediction were performed. Finally, the cytotoxicity studies were performed for the most active compounds using MTT assay against normal MRC5 cells.
PB  - Basel: MDPI
T2  - Pharmaceuticals
T1  - N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation
IS  - 1
VL  - 16
DO  - 10.3390/ph16010131
SP  - 131
ER  - 

@article{
author = "Petrou, Anthi and Geronikaki, Athina and Kartsev, Victor and Kousaxidis, Antonios and Papadimitriou-Tsantarliotou, Aliki and Kostić, Marina and Ivanov, Marija and Soković, Marina and Nicolaou, Ioannis and Vizirianakis, Ioannis S.",
year = "2023",
abstract = "Herein, we report the experimental evaluation of the antimicrobial activity of seventeen new (Z)-methyl 3-(4-oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylate derivatives. All tested compounds exhibited antibacterial activity against eight Gram-positive and Gram-negative bacteria. Their activity exceeded those of ampicillin as well as streptomycin by 10-50 fold. The most sensitive bacterium was En. Cloacae, while E. coli was the most resistant one, followed by M. flavus. The most active compound appeared to be compound 8 with MIC at 0.004-0.03 mg/mL and MBC at 0.008-0.06 mg/mL. The antifungal activity of tested compounds was good to excellent with MIC in the range of 0.004-0.06 mg/mL, with compound 15 being the most potent. T. viride was the most sensitive fungal, while A. fumigatus was the most resistant one. Docking studies revealed that the inhibition of E. coli MurB is probably responsible for their antibacterial activity, while 14a-lanosterol demethylase of CYP51Ca is involved in the mechanism of antifungal activity. Furthermore, drug-likeness and ADMET profile prediction were performed. Finally, the cytotoxicity studies were performed for the most active compounds using MTT assay against normal MRC5 cells.",
publisher = "Basel: MDPI",
journal = "Pharmaceuticals",
title = "N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation",
number = "1",
volume = "16",
doi = "10.3390/ph16010131",
pages = "131"
}

Petrou, A., Geronikaki, A., Kartsev, V., Kousaxidis, A., Papadimitriou-Tsantarliotou, A., Kostić, M., Ivanov, M., Soković, M., Nicolaou, I.,& Vizirianakis, I. S.. (2023). N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation. in Pharmaceuticals
Basel: MDPI., 16(1), 131.
https://doi.org/10.3390/ph16010131

Petrou A, Geronikaki A, Kartsev V, Kousaxidis A, Papadimitriou-Tsantarliotou A, Kostić M, Ivanov M, Soković M, Nicolaou I, Vizirianakis IS. N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation. in Pharmaceuticals. 2023;16(1):131.
doi:10.3390/ph16010131 .

Petrou, Anthi, Geronikaki, Athina, Kartsev, Victor, Kousaxidis, Antonios, Papadimitriou-Tsantarliotou, Aliki, Kostić, Marina, Ivanov, Marija, Soković, Marina, Nicolaou, Ioannis, Vizirianakis, Ioannis S., "N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation" in Pharmaceuticals, 16, no. 1 (2023):131,
https://doi.org/10.3390/ph16010131 . .

TY  - JOUR
AU  - Kartsev, Victor
AU  - Geronikaki, Athina
AU  - Lichitsky, Boris
AU  - Komogortsev, Andrey
AU  - Petrou, Anthi
AU  - Ivanov, Marija
AU  - Glamočlija, Jasmina
AU  - Soković, Marina
PY  - 2022
UR  - https://onlinelibrary.wiley.com/doi/10.1002/jhet.4491
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/4962
AB  - Herein we report the design and synthesis of thiazolo[4,5-b]pyridin-5-ones and evaluation of their antimicrobial activity. The design was based on a molecular hybridization approach. Evaluation of their antibacterial activity revealed that these compounds generally showed moderate antibacterial activity. The best activity was achieved for compound 4p with MIC/MBC in the range of 0.12-0.47 and 0.23-0.94 mg mL(-1) respectively. Three compounds (4g, 4n, and 4p) were tested against three resistant strains, namely MRSA, p.aeruginosa, and E.coli, showing higher inhibition potential than the reference drug ampicillin. These three compounds also were tested for their ability to inhibit biofilm formation, with two of them showing better activity than streptomycin in a concentration of MIC (4p) and ampicillin in both concentrations (MIC and 0.5 MIC). As far as antifungal activity is concerned, the best activity was observed for compound 4i with MIC at 0.12-0.47 mg mL(-1) and MFC at 0.23-0.94 mg m(-1). According to docking studies, the predicted inhibition of E.coli MurB enzyme is probably a putative mechanism of the antibacterial activity of these compounds, while inhibition of 14a-lanosterol demethylase is probably the mechanism of their antifungal activity.
T2  - Journal of Heterocyclic Chemistry
T1  - Synthesis, biological evaluation and molecular docking studies of thiazolo[4,5‐ b ]pyridin‐5‐ones as antimicrobial agents
IS  - 9
VL  - 59
DO  - 10.1002/jhet.4491
SP  - 1573
EP  - 1590
ER  - 

@article{
author = "Kartsev, Victor and Geronikaki, Athina and Lichitsky, Boris and Komogortsev, Andrey and Petrou, Anthi and Ivanov, Marija and Glamočlija, Jasmina and Soković, Marina",
year = "2022",
abstract = "Herein we report the design and synthesis of thiazolo[4,5-b]pyridin-5-ones and evaluation of their antimicrobial activity. The design was based on a molecular hybridization approach. Evaluation of their antibacterial activity revealed that these compounds generally showed moderate antibacterial activity. The best activity was achieved for compound 4p with MIC/MBC in the range of 0.12-0.47 and 0.23-0.94 mg mL(-1) respectively. Three compounds (4g, 4n, and 4p) were tested against three resistant strains, namely MRSA, p.aeruginosa, and E.coli, showing higher inhibition potential than the reference drug ampicillin. These three compounds also were tested for their ability to inhibit biofilm formation, with two of them showing better activity than streptomycin in a concentration of MIC (4p) and ampicillin in both concentrations (MIC and 0.5 MIC). As far as antifungal activity is concerned, the best activity was observed for compound 4i with MIC at 0.12-0.47 mg mL(-1) and MFC at 0.23-0.94 mg m(-1). According to docking studies, the predicted inhibition of E.coli MurB enzyme is probably a putative mechanism of the antibacterial activity of these compounds, while inhibition of 14a-lanosterol demethylase is probably the mechanism of their antifungal activity.",
journal = "Journal of Heterocyclic Chemistry",
title = "Synthesis, biological evaluation and molecular docking studies of thiazolo[4,5‐ b ]pyridin‐5‐ones as antimicrobial agents",
number = "9",
volume = "59",
doi = "10.1002/jhet.4491",
pages = "1573-1590"
}

Kartsev, V., Geronikaki, A., Lichitsky, B., Komogortsev, A., Petrou, A., Ivanov, M., Glamočlija, J.,& Soković, M.. (2022). Synthesis, biological evaluation and molecular docking studies of thiazolo[4,5‐ b ]pyridin‐5‐ones as antimicrobial agents. in Journal of Heterocyclic Chemistry, 59(9), 1573-1590.
https://doi.org/10.1002/jhet.4491

Kartsev V, Geronikaki A, Lichitsky B, Komogortsev A, Petrou A, Ivanov M, Glamočlija J, Soković M. Synthesis, biological evaluation and molecular docking studies of thiazolo[4,5‐ b ]pyridin‐5‐ones as antimicrobial agents. in Journal of Heterocyclic Chemistry. 2022;59(9):1573-1590.
doi:10.1002/jhet.4491 .

Kartsev, Victor, Geronikaki, Athina, Lichitsky, Boris, Komogortsev, Andrey, Petrou, Anthi, Ivanov, Marija, Glamočlija, Jasmina, Soković, Marina, "Synthesis, biological evaluation and molecular docking studies of thiazolo[4,5‐ b ]pyridin‐5‐ones as antimicrobial agents" in Journal of Heterocyclic Chemistry, 59, no. 9 (2022):1573-1590,
https://doi.org/10.1002/jhet.4491 . .

TY  - JOUR
AU  - Zubenko, Alexander
AU  - Kartsev, Victor
AU  - Petrou, Anthi
AU  - Geronikaki, Athina
AU  - Ivanov, Marija
AU  - Glamočlija, Jasmina
AU  - Soković, Marina
AU  - Divaeva, Lyudmila
AU  - Morkovnik, Anatolii
AU  - Klimenko, Alexander
PY  - 2022
UR  - https://www.mdpi.com/2079-6382/11/11/1654
UR  - http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC9686863
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/5399
AB  - In this manuscript, we describe the design, preparation, and studies of antimicrobial activity of a series of novel heteroarylated benzothiazoles. A molecular hybridization approach was used for the designing compounds. The in vitro evaluation exposed that these compounds showed moderate antibacterial activity. Compound 2j was found to be the most potent (MIC/MBC at 0.23-0.94 mg/mL and 0.47-1.88 mg/mL) On the other hand, compounds showed good antifungal activity (MIC/MFC at 0.06-0.47 and 0.11-0.94 mg/mL respectively) with 2d being the most active one. The docking studies revealed that inhibition of E. coli MurB and 14-lanosterol demethylase probably represent the mechanism of antibacterial and antifungal activities.
PB  - Basel: MDPI
T2  - Antibiotics
T1  - Experimental and In Silico Evaluation of New Heteroaryl Benzothiazole Derivatives as Antimicrobial Agents
IS  - 11
VL  - 11
DO  - 10.3390/antibiotics11111654
SP  - 1654
ER  - 

@article{
author = "Zubenko, Alexander and Kartsev, Victor and Petrou, Anthi and Geronikaki, Athina and Ivanov, Marija and Glamočlija, Jasmina and Soković, Marina and Divaeva, Lyudmila and Morkovnik, Anatolii and Klimenko, Alexander",
year = "2022",
abstract = "In this manuscript, we describe the design, preparation, and studies of antimicrobial activity of a series of novel heteroarylated benzothiazoles. A molecular hybridization approach was used for the designing compounds. The in vitro evaluation exposed that these compounds showed moderate antibacterial activity. Compound 2j was found to be the most potent (MIC/MBC at 0.23-0.94 mg/mL and 0.47-1.88 mg/mL) On the other hand, compounds showed good antifungal activity (MIC/MFC at 0.06-0.47 and 0.11-0.94 mg/mL respectively) with 2d being the most active one. The docking studies revealed that inhibition of E. coli MurB and 14-lanosterol demethylase probably represent the mechanism of antibacterial and antifungal activities.",
publisher = "Basel: MDPI",
journal = "Antibiotics",
title = "Experimental and In Silico Evaluation of New Heteroaryl Benzothiazole Derivatives as Antimicrobial Agents",
number = "11",
volume = "11",
doi = "10.3390/antibiotics11111654",
pages = "1654"
}

Zubenko, A., Kartsev, V., Petrou, A., Geronikaki, A., Ivanov, M., Glamočlija, J., Soković, M., Divaeva, L., Morkovnik, A.,& Klimenko, A.. (2022). Experimental and In Silico Evaluation of New Heteroaryl Benzothiazole Derivatives as Antimicrobial Agents. in Antibiotics
Basel: MDPI., 11(11), 1654.
https://doi.org/10.3390/antibiotics11111654

Zubenko A, Kartsev V, Petrou A, Geronikaki A, Ivanov M, Glamočlija J, Soković M, Divaeva L, Morkovnik A, Klimenko A. Experimental and In Silico Evaluation of New Heteroaryl Benzothiazole Derivatives as Antimicrobial Agents. in Antibiotics. 2022;11(11):1654.
doi:10.3390/antibiotics11111654 .

Zubenko, Alexander, Kartsev, Victor, Petrou, Anthi, Geronikaki, Athina, Ivanov, Marija, Glamočlija, Jasmina, Soković, Marina, Divaeva, Lyudmila, Morkovnik, Anatolii, Klimenko, Alexander, "Experimental and In Silico Evaluation of New Heteroaryl Benzothiazole Derivatives as Antimicrobial Agents" in Antibiotics, 11, no. 11 (2022):1654,
https://doi.org/10.3390/antibiotics11111654 . .

TY  - JOUR
AU  - Kartsev, Victor
AU  - Geronikaki, Athina
AU  - Zubenko, Alexander
AU  - Petrou, Anthi
AU  - Ivanov, Marija
AU  - Glamočlija, Jasmina
AU  - Soković, Marina
AU  - Divaeva, Lyudmila
AU  - Morkovnik, Anatolii
AU  - Klimenko, Alexander
PY  - 2022
UR  - http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC9658463
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/5173
AB  - Herein, we report the design, synthesis, and evaluation of the antimicrobial activity of new heteroaryl (aryl) thiazole derivatives. The design was based on a molecular hybridization approach. The in vitro evaluation revealed that these compounds demonstrated moderate antibacterial activity. The best activity was achieved for compound 3, with MIC and MBC in the range of 0.23-0.7 and 0.47-0.94 mg/mL, respectively. Three compounds (2, 3, and 4) were tested against three resistant strains, namely methicillin resistant Staphylococcus aureus, P. aeruginosa, and E. coli, which showed higher potential than the reference drug ampicillin. Antifungal activity of the compounds was better with MIC and MFC in the range of 0.06-0.47 and 0.11-0.94 mg/mL, respectively. The best activity was observed for compound 9, with MIC at 0.06-0.23 mg/mL and MFC at 0.11-0.47 mg/mL. According to docking studies, the predicted inhibition of the E. coli MurB enzyme is a putative mechanism of the antibacterial activity of the compounds, while inhibition of 14a-lanosterol demethylase is probably the mechanism of their antifungal activity.
PB  - Basel: MDPI
T2  - Antibiotics
T1  - Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies
IS  - 10
VL  - 11
DO  - 10.3390/antibiotics11101337
SP  - 1337
ER  - 

@article{
author = "Kartsev, Victor and Geronikaki, Athina and Zubenko, Alexander and Petrou, Anthi and Ivanov, Marija and Glamočlija, Jasmina and Soković, Marina and Divaeva, Lyudmila and Morkovnik, Anatolii and Klimenko, Alexander",
year = "2022",
abstract = "Herein, we report the design, synthesis, and evaluation of the antimicrobial activity of new heteroaryl (aryl) thiazole derivatives. The design was based on a molecular hybridization approach. The in vitro evaluation revealed that these compounds demonstrated moderate antibacterial activity. The best activity was achieved for compound 3, with MIC and MBC in the range of 0.23-0.7 and 0.47-0.94 mg/mL, respectively. Three compounds (2, 3, and 4) were tested against three resistant strains, namely methicillin resistant Staphylococcus aureus, P. aeruginosa, and E. coli, which showed higher potential than the reference drug ampicillin. Antifungal activity of the compounds was better with MIC and MFC in the range of 0.06-0.47 and 0.11-0.94 mg/mL, respectively. The best activity was observed for compound 9, with MIC at 0.06-0.23 mg/mL and MFC at 0.11-0.47 mg/mL. According to docking studies, the predicted inhibition of the E. coli MurB enzyme is a putative mechanism of the antibacterial activity of the compounds, while inhibition of 14a-lanosterol demethylase is probably the mechanism of their antifungal activity.",
publisher = "Basel: MDPI",
journal = "Antibiotics",
title = "Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies",
number = "10",
volume = "11",
doi = "10.3390/antibiotics11101337",
pages = "1337"
}

Kartsev, V., Geronikaki, A., Zubenko, A., Petrou, A., Ivanov, M., Glamočlija, J., Soković, M., Divaeva, L., Morkovnik, A.,& Klimenko, A.. (2022). Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies. in Antibiotics
Basel: MDPI., 11(10), 1337.
https://doi.org/10.3390/antibiotics11101337

Kartsev V, Geronikaki A, Zubenko A, Petrou A, Ivanov M, Glamočlija J, Soković M, Divaeva L, Morkovnik A, Klimenko A. Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies. in Antibiotics. 2022;11(10):1337.
doi:10.3390/antibiotics11101337 .

Kartsev, Victor, Geronikaki, Athina, Zubenko, Alexander, Petrou, Anthi, Ivanov, Marija, Glamočlija, Jasmina, Soković, Marina, Divaeva, Lyudmila, Morkovnik, Anatolii, Klimenko, Alexander, "Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies" in Antibiotics, 11, no. 10 (2022):1337,
https://doi.org/10.3390/antibiotics11101337 . .

TY  - JOUR
AU  - Horishny, Volodymyr
AU  - Geronikaki, Athina
AU  - Kartsev, Victor
AU  - Matiychuk, Vasyl
AU  - Petrou, Anthi
AU  - Pogodin, Pavel
AU  - Poroikov, Vladimir
AU  - Papadopoulou, Theodora A
AU  - Vizirianakis, Ioannis S
AU  - Kostić, Marina
AU  - Ivanov, Marija
AU  - Soković, Marina
PY  - 2022
UR  - http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC8839324
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/4884
AB  - BACKGROUND Infectious diseases represent a significant global strain on public health security and impact on socio-economic stability all over the world. The increasing resistance to the current antimicrobial treatment has resulted in the crucial need for the discovery and development of novel entities for the infectious treatment with different modes of action that could target both sensitive and resistant strains. METHODS Compounds were synthesized using the classical organic chemistry methods. Prediction of biological activity spectra was carried out using PASS and PASS-based web applications. Pharmacophore modeling in LigandScout software was used for quantitative modeling of the antibacterial activity. Antimicrobial activity was evaluated using the microdilution method. AutoDock 4.2® software was used to elucidate probable bacterial and fungal molecular targets of the studied compounds. RESULTS All compounds exhibited better antibacterial potency than ampicillin against all bacteria tested. Three compounds were tested against resistant strains MRSA, P. aeruginosa and E. coli and were found to be more potent than MRSA than reference drugs. All compounds demonstrated a higher degree of antifungal activity than the reference drugs bifonazole (6-17-fold) and ketoconazole (13-52-fold). Three of the most active compounds could be considered for further development of the new, more potent antimicrobial agents. CONCLUSION Compounds 5b (Z)-3-(3-hydroxyphenyl)-5-((1-methyl-1H-indol-3-yl)methylene)-2-thioxothiazolidin-4-one and 5g (Z)-3-[5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-benzoic acid as well as 5h (Z)-3-(5-((5-methoxy-1H-indol-3-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzoic acid can be considered as lead compounds for further development of more potent and safe antibacterial and antifungal agents.
PB  - Basel: MDPI
T2  - Molecules
T1  - Synthesis, Biological Evaluation and Molecular Docking Studies of 5-Indolylmethylen-4-oxo-2-thioxothiazolidine Derivatives.
IS  - 3
VL  - 27
DO  - 10.3390/molecules27031068
SP  - 1068
ER  - 

@article{
author = "Horishny, Volodymyr and Geronikaki, Athina and Kartsev, Victor and Matiychuk, Vasyl and Petrou, Anthi and Pogodin, Pavel and Poroikov, Vladimir and Papadopoulou, Theodora A and Vizirianakis, Ioannis S and Kostić, Marina and Ivanov, Marija and Soković, Marina",
year = "2022",
abstract = "BACKGROUND Infectious diseases represent a significant global strain on public health security and impact on socio-economic stability all over the world. The increasing resistance to the current antimicrobial treatment has resulted in the crucial need for the discovery and development of novel entities for the infectious treatment with different modes of action that could target both sensitive and resistant strains. METHODS Compounds were synthesized using the classical organic chemistry methods. Prediction of biological activity spectra was carried out using PASS and PASS-based web applications. Pharmacophore modeling in LigandScout software was used for quantitative modeling of the antibacterial activity. Antimicrobial activity was evaluated using the microdilution method. AutoDock 4.2® software was used to elucidate probable bacterial and fungal molecular targets of the studied compounds. RESULTS All compounds exhibited better antibacterial potency than ampicillin against all bacteria tested. Three compounds were tested against resistant strains MRSA, P. aeruginosa and E. coli and were found to be more potent than MRSA than reference drugs. All compounds demonstrated a higher degree of antifungal activity than the reference drugs bifonazole (6-17-fold) and ketoconazole (13-52-fold). Three of the most active compounds could be considered for further development of the new, more potent antimicrobial agents. CONCLUSION Compounds 5b (Z)-3-(3-hydroxyphenyl)-5-((1-methyl-1H-indol-3-yl)methylene)-2-thioxothiazolidin-4-one and 5g (Z)-3-[5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-benzoic acid as well as 5h (Z)-3-(5-((5-methoxy-1H-indol-3-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzoic acid can be considered as lead compounds for further development of more potent and safe antibacterial and antifungal agents.",
publisher = "Basel: MDPI",
journal = "Molecules",
title = "Synthesis, Biological Evaluation and Molecular Docking Studies of 5-Indolylmethylen-4-oxo-2-thioxothiazolidine Derivatives.",
number = "3",
volume = "27",
doi = "10.3390/molecules27031068",
pages = "1068"
}

Horishny, V., Geronikaki, A., Kartsev, V., Matiychuk, V., Petrou, A., Pogodin, P., Poroikov, V., Papadopoulou, T. A., Vizirianakis, I. S., Kostić, M., Ivanov, M.,& Soković, M.. (2022). Synthesis, Biological Evaluation and Molecular Docking Studies of 5-Indolylmethylen-4-oxo-2-thioxothiazolidine Derivatives.. in Molecules
Basel: MDPI., 27(3), 1068.
https://doi.org/10.3390/molecules27031068

Horishny V, Geronikaki A, Kartsev V, Matiychuk V, Petrou A, Pogodin P, Poroikov V, Papadopoulou TA, Vizirianakis IS, Kostić M, Ivanov M, Soković M. Synthesis, Biological Evaluation and Molecular Docking Studies of 5-Indolylmethylen-4-oxo-2-thioxothiazolidine Derivatives.. in Molecules. 2022;27(3):1068.
doi:10.3390/molecules27031068 .

Horishny, Volodymyr, Geronikaki, Athina, Kartsev, Victor, Matiychuk, Vasyl, Petrou, Anthi, Pogodin, Pavel, Poroikov, Vladimir, Papadopoulou, Theodora A, Vizirianakis, Ioannis S, Kostić, Marina, Ivanov, Marija, Soković, Marina, "Synthesis, Biological Evaluation and Molecular Docking Studies of 5-Indolylmethylen-4-oxo-2-thioxothiazolidine Derivatives." in Molecules, 27, no. 3 (2022):1068,
https://doi.org/10.3390/molecules27031068 . .

TY  - JOUR
AU  - Sirakanyan, Samvel
AU  - Kartsev, Victor
AU  - Spinelli, Domenico
AU  - Geronikaki, Athina
AU  - Petrou, Anthi
AU  - Ivanov, Marija
AU  - Glamočlija, Jasmina
AU  - Soković, Marina
AU  - Hakobyan, Elmira
AU  - Hovakimyan, Anush
PY  - 2021
UR  - https://onlinelibrary.wiley.com/doi/10.1002/ardp.202000208
UR  - http://www.ncbi.nlm.nih.gov/pubmed/33029832
UR  - https://radar.ibiss.bg.ac.rs/123456789/3916
AB  - In this study, we report the synthesis and antimicrobial activity of some new disubstituted piperazines. Thus, 3-chlorocyclopenta[c]pyridines and 6-chloropyrano[3,4-c]pyridine 1 under mild reaction conditions with piperazine gave the 3(6)-piperazine-substituted cyclopenta[c]pyridines and pyrano[3,4-c]pyridine 2. Furthermore, the latter, by alkylation with 2-chloro-N-1,3-thiazol-2-ylacetamide, led to the formation of the target compounds. The evaluation of the antibacterial activity revealed that 3k was the most potent compound. The most sensitive bacterium was found to be Listeria monocytogenes, whereas Staphylococcus aureus was the most resistant one. Three compounds, 3d, 3g, and 3k, were tested also against the following resistant strains: methicillin-resistant S. aureus (MRSA), Escherichia coli, and Pseudomonas aeruginosa. All three compounds appeared to be more potent than ampicillin against MRSA. Moreover, compound 3d showed a better activity than the reference drug ampicillin against P. aeruginosa, whereas 3g was more efficient against E. coli. The best antifungal activity was observed again for compound 3k. The most resistant fungi appeared to be Aspergillus fumigatus, whereas Trichoderma viride seemed the most sensitive one toward the compounds tested. Molecular docking studies on E. coli MurB, as well as on Candida albicans CYP51 and dihydrofolate reductase, were used for the prediction of the mechanisms of the antibacterial and antifungal activities, confirming the experimental results.
PB  - Wiley-VCH Verlag
T2  - Archiv der Pharmazie
T1  - Synthesis and antimicrobial activity of new 2-piperazin-1-yl-N-1,3-thiazol-2-ylacetamides of cyclopenta[c]pyridines and pyrano[3,4-c]pyridines.
IS  - 1
VL  - 354
DO  - 10.1002/ardp.202000208
SP  - e2000208
SP  - 2000208
ER  - 

@article{
author = "Sirakanyan, Samvel and Kartsev, Victor and Spinelli, Domenico and Geronikaki, Athina and Petrou, Anthi and Ivanov, Marija and Glamočlija, Jasmina and Soković, Marina and Hakobyan, Elmira and Hovakimyan, Anush",
year = "2021",
abstract = "In this study, we report the synthesis and antimicrobial activity of some new disubstituted piperazines. Thus, 3-chlorocyclopenta[c]pyridines and 6-chloropyrano[3,4-c]pyridine 1 under mild reaction conditions with piperazine gave the 3(6)-piperazine-substituted cyclopenta[c]pyridines and pyrano[3,4-c]pyridine 2. Furthermore, the latter, by alkylation with 2-chloro-N-1,3-thiazol-2-ylacetamide, led to the formation of the target compounds. The evaluation of the antibacterial activity revealed that 3k was the most potent compound. The most sensitive bacterium was found to be Listeria monocytogenes, whereas Staphylococcus aureus was the most resistant one. Three compounds, 3d, 3g, and 3k, were tested also against the following resistant strains: methicillin-resistant S. aureus (MRSA), Escherichia coli, and Pseudomonas aeruginosa. All three compounds appeared to be more potent than ampicillin against MRSA. Moreover, compound 3d showed a better activity than the reference drug ampicillin against P. aeruginosa, whereas 3g was more efficient against E. coli. The best antifungal activity was observed again for compound 3k. The most resistant fungi appeared to be Aspergillus fumigatus, whereas Trichoderma viride seemed the most sensitive one toward the compounds tested. Molecular docking studies on E. coli MurB, as well as on Candida albicans CYP51 and dihydrofolate reductase, were used for the prediction of the mechanisms of the antibacterial and antifungal activities, confirming the experimental results.",
publisher = "Wiley-VCH Verlag",
journal = "Archiv der Pharmazie",
title = "Synthesis and antimicrobial activity of new 2-piperazin-1-yl-N-1,3-thiazol-2-ylacetamides of cyclopenta[c]pyridines and pyrano[3,4-c]pyridines.",
number = "1",
volume = "354",
doi = "10.1002/ardp.202000208",
pages = "e2000208-2000208"
}

Sirakanyan, S., Kartsev, V., Spinelli, D., Geronikaki, A., Petrou, A., Ivanov, M., Glamočlija, J., Soković, M., Hakobyan, E.,& Hovakimyan, A.. (2021). Synthesis and antimicrobial activity of new 2-piperazin-1-yl-N-1,3-thiazol-2-ylacetamides of cyclopenta[c]pyridines and pyrano[3,4-c]pyridines.. in Archiv der Pharmazie
Wiley-VCH Verlag., 354(1), e2000208.
https://doi.org/10.1002/ardp.202000208

Sirakanyan S, Kartsev V, Spinelli D, Geronikaki A, Petrou A, Ivanov M, Glamočlija J, Soković M, Hakobyan E, Hovakimyan A. Synthesis and antimicrobial activity of new 2-piperazin-1-yl-N-1,3-thiazol-2-ylacetamides of cyclopenta[c]pyridines and pyrano[3,4-c]pyridines.. in Archiv der Pharmazie. 2021;354(1):e2000208.
doi:10.1002/ardp.202000208 .

Sirakanyan, Samvel, Kartsev, Victor, Spinelli, Domenico, Geronikaki, Athina, Petrou, Anthi, Ivanov, Marija, Glamočlija, Jasmina, Soković, Marina, Hakobyan, Elmira, Hovakimyan, Anush, "Synthesis and antimicrobial activity of new 2-piperazin-1-yl-N-1,3-thiazol-2-ylacetamides of cyclopenta[c]pyridines and pyrano[3,4-c]pyridines." in Archiv der Pharmazie, 354, no. 1 (2021):e2000208,
https://doi.org/10.1002/ardp.202000208 . .

TY  - JOUR
AU  - Simakov, Sergei
AU  - Kartsev, Victor
AU  - Petrou, Anthi
AU  - Nicolaou, Ioannis
AU  - Geronikaki, Athina
AU  - Ivanov, Marija
AU  - Kostić, Marina
AU  - Glamočlija, Jasmina
AU  - Soković, Marina
AU  - Talea, Despoina
AU  - Vizirianakis, Ioannis S.
PY  - 2021
UR  - https://www.mdpi.com/1424-8247/14/11/1096
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/4663
AB  - This manuscript deals with the synthesis and computational and experimental evaluation of the antimicrobial activity of twenty-nine 4-(indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole acylamines. An evaluation of antibacterial activity against Gram (+) and Gram (−) bacteria revealed that the MIC of indole derivatives is in the range of 0.06–1.88 mg/mL, while among fourteen methylindole derivatives, only six were active, with an MIC in the range of of 0.47–1.88 mg/mL. S. aureus appeared to be the most resistant strain, while S. Typhimurium was the most sensitive. Compound 5x was the most promising, with an MIC in the range of 0.06–0.12 mg/mL, followed by 5d and 5m. An evaluation of these three compounds against resistant strains, namely MRSA P. aeruginosa and E. coli, revealed that they were more potent against MRSA than ampicillin. Furthermore, compounds 5m and 5x were superior inhibitors of biofilm formation, compared to ampicillin and streptomycin, in terms Compounds 5d, 5m, and 5x interact with streptomycin in additive manner. The antifungal activity of some compounds exceeded or was equipotent to those of the reference antifungal agents bifonazole and ketoconazole. The most potent antifungal agent was found to be compound 5g. Drug likeness scores of compounds was in a range of −0.63 to 0.29, which is moderate to good. According to docking studies, E. coli MurB inhibition is probably responsible for the antibacterial activity of compounds, whereas CYP51 inhibition was implicated in antifungal activity. Compounds appeared to be non-toxic, according to the cytotoxicity assessment in MRC-5 cells.
PB  - Basel: MDPI
T2  - Pharmaceuticals
T1  - 4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation
IS  - 11
VL  - 14
DO  - 10.3390/ph14111096
SP  - 1096
ER  - 

@article{
author = "Simakov, Sergei and Kartsev, Victor and Petrou, Anthi and Nicolaou, Ioannis and Geronikaki, Athina and Ivanov, Marija and Kostić, Marina and Glamočlija, Jasmina and Soković, Marina and Talea, Despoina and Vizirianakis, Ioannis S.",
year = "2021",
abstract = "This manuscript deals with the synthesis and computational and experimental evaluation of the antimicrobial activity of twenty-nine 4-(indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole acylamines. An evaluation of antibacterial activity against Gram (+) and Gram (−) bacteria revealed that the MIC of indole derivatives is in the range of 0.06–1.88 mg/mL, while among fourteen methylindole derivatives, only six were active, with an MIC in the range of of 0.47–1.88 mg/mL. S. aureus appeared to be the most resistant strain, while S. Typhimurium was the most sensitive. Compound 5x was the most promising, with an MIC in the range of 0.06–0.12 mg/mL, followed by 5d and 5m. An evaluation of these three compounds against resistant strains, namely MRSA P. aeruginosa and E. coli, revealed that they were more potent against MRSA than ampicillin. Furthermore, compounds 5m and 5x were superior inhibitors of biofilm formation, compared to ampicillin and streptomycin, in terms Compounds 5d, 5m, and 5x interact with streptomycin in additive manner. The antifungal activity of some compounds exceeded or was equipotent to those of the reference antifungal agents bifonazole and ketoconazole. The most potent antifungal agent was found to be compound 5g. Drug likeness scores of compounds was in a range of −0.63 to 0.29, which is moderate to good. According to docking studies, E. coli MurB inhibition is probably responsible for the antibacterial activity of compounds, whereas CYP51 inhibition was implicated in antifungal activity. Compounds appeared to be non-toxic, according to the cytotoxicity assessment in MRC-5 cells.",
publisher = "Basel: MDPI",
journal = "Pharmaceuticals",
title = "4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation",
number = "11",
volume = "14",
doi = "10.3390/ph14111096",
pages = "1096"
}

Simakov, S., Kartsev, V., Petrou, A., Nicolaou, I., Geronikaki, A., Ivanov, M., Kostić, M., Glamočlija, J., Soković, M., Talea, D.,& Vizirianakis, I. S.. (2021). 4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation. in Pharmaceuticals
Basel: MDPI., 14(11), 1096.
https://doi.org/10.3390/ph14111096

Simakov S, Kartsev V, Petrou A, Nicolaou I, Geronikaki A, Ivanov M, Kostić M, Glamočlija J, Soković M, Talea D, Vizirianakis IS. 4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation. in Pharmaceuticals. 2021;14(11):1096.
doi:10.3390/ph14111096 .

Simakov, Sergei, Kartsev, Victor, Petrou, Anthi, Nicolaou, Ioannis, Geronikaki, Athina, Ivanov, Marija, Kostić, Marina, Glamočlija, Jasmina, Soković, Marina, Talea, Despoina, Vizirianakis, Ioannis S., "4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation" in Pharmaceuticals, 14, no. 11 (2021):1096,
https://doi.org/10.3390/ph14111096 . .

TY  - JOUR
AU  - Geronikaki, Athina
AU  - Kartsev, Victor
AU  - Eleftheriou, Phaedra
AU  - Petrou, Anthi
AU  - Glamočlija, Jasmina
AU  - Ćirić, Ana
AU  - Soković, Marina
PY  - 2020
UR  - https://www.eurekaselect.com/186178/article
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/4000
AB  - Background: Although a great number of the targets of antimicrobial therapy have been achieved, it remains among the first fields of pharmaceutical research, mainly because of the development of resistant strains. Docking analysis may be an important tool in the research for the development of more effective agents against specific drug targets or multi-target agents 1-3. Methods: In the present study, based on docking analysis, ten tetrahydrothiazolo[2,3-a]isoindole derivatives were chosen for the evaluation of the antimicrobial activity. Results: All compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species being, in some cases, more potent than ampicillin and streptomycin against all species. The most sensitive bacteria appeared to be S. aureus and En. Cloacae, while M. flavus, E. coli and P. aeruginosa were the most resistant ones. The compounds were also tested for their antifungal activity against eight fungal species. All compounds exhibited good antifungal activity better than reference drugs bifonazole (1.4 – 41 folds) and ketoconazole (1.1 – 406 folds) against all fungal species. In order to elucidate the mechanism of action, docking studies on different antimicrobial targets were performed. Conclusion: According to docking analysis, the antifungal activity can be explained by the inhibition of the CYP51 enzyme for most compounds with a better correlation of the results obtained for the P.v.c. strain (linear regression between estimated binding Energy and log(1/MIC) with R 2 =0.867 and p=0.000091 or R 2 = 0.924, p= 0.000036, when compound 3 is excluded.
PB  - Bentham Science Publishers Ltd.
T2  - Current Topics in Medicinal Chemistry
T1  - Substituted 6,7-dimethoxy-5-oxo-2,3,5,9b-tetrahydrothiazolo[2,3-a]isoindole-3-1,1-dioxidederivatives with antimicrobial activity and docking assisted prediction of the mechanism of their antibacterial and antifungal properties
IS  - 29
VL  - 20
DO  - 10.2174/1568026620666200922114735
SP  - 2681
EP  - 2691
ER  - 

@article{
author = "Geronikaki, Athina and Kartsev, Victor and Eleftheriou, Phaedra and Petrou, Anthi and Glamočlija, Jasmina and Ćirić, Ana and Soković, Marina",
year = "2020",
abstract = "Background: Although a great number of the targets of antimicrobial therapy have been achieved, it remains among the first fields of pharmaceutical research, mainly because of the development of resistant strains. Docking analysis may be an important tool in the research for the development of more effective agents against specific drug targets or multi-target agents 1-3. Methods: In the present study, based on docking analysis, ten tetrahydrothiazolo[2,3-a]isoindole derivatives were chosen for the evaluation of the antimicrobial activity. Results: All compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species being, in some cases, more potent than ampicillin and streptomycin against all species. The most sensitive bacteria appeared to be S. aureus and En. Cloacae, while M. flavus, E. coli and P. aeruginosa were the most resistant ones. The compounds were also tested for their antifungal activity against eight fungal species. All compounds exhibited good antifungal activity better than reference drugs bifonazole (1.4 – 41 folds) and ketoconazole (1.1 – 406 folds) against all fungal species. In order to elucidate the mechanism of action, docking studies on different antimicrobial targets were performed. Conclusion: According to docking analysis, the antifungal activity can be explained by the inhibition of the CYP51 enzyme for most compounds with a better correlation of the results obtained for the P.v.c. strain (linear regression between estimated binding Energy and log(1/MIC) with R 2 =0.867 and p=0.000091 or R 2 = 0.924, p= 0.000036, when compound 3 is excluded.",
publisher = "Bentham Science Publishers Ltd.",
journal = "Current Topics in Medicinal Chemistry",
title = "Substituted 6,7-dimethoxy-5-oxo-2,3,5,9b-tetrahydrothiazolo[2,3-a]isoindole-3-1,1-dioxidederivatives with antimicrobial activity and docking assisted prediction of the mechanism of their antibacterial and antifungal properties",
number = "29",
volume = "20",
doi = "10.2174/1568026620666200922114735",
pages = "2681-2691"
}

Geronikaki, A., Kartsev, V., Eleftheriou, P., Petrou, A., Glamočlija, J., Ćirić, A.,& Soković, M.. (2020). Substituted 6,7-dimethoxy-5-oxo-2,3,5,9b-tetrahydrothiazolo[2,3-a]isoindole-3-1,1-dioxidederivatives with antimicrobial activity and docking assisted prediction of the mechanism of their antibacterial and antifungal properties. in Current Topics in Medicinal Chemistry
Bentham Science Publishers Ltd.., 20(29), 2681-2691.
https://doi.org/10.2174/1568026620666200922114735

Geronikaki A, Kartsev V, Eleftheriou P, Petrou A, Glamočlija J, Ćirić A, Soković M. Substituted 6,7-dimethoxy-5-oxo-2,3,5,9b-tetrahydrothiazolo[2,3-a]isoindole-3-1,1-dioxidederivatives with antimicrobial activity and docking assisted prediction of the mechanism of their antibacterial and antifungal properties. in Current Topics in Medicinal Chemistry. 2020;20(29):2681-2691.
doi:10.2174/1568026620666200922114735 .

Geronikaki, Athina, Kartsev, Victor, Eleftheriou, Phaedra, Petrou, Anthi, Glamočlija, Jasmina, Ćirić, Ana, Soković, Marina, "Substituted 6,7-dimethoxy-5-oxo-2,3,5,9b-tetrahydrothiazolo[2,3-a]isoindole-3-1,1-dioxidederivatives with antimicrobial activity and docking assisted prediction of the mechanism of their antibacterial and antifungal properties" in Current Topics in Medicinal Chemistry, 20, no. 29 (2020):2681-2691,
https://doi.org/10.2174/1568026620666200922114735 . .

TY  - JOUR
AU  - Horishny, Volodymyr
AU  - Kartsev, Victor
AU  - Matiychuk, Vasyl
AU  - Geronikaki, Athina
AU  - Anthi, Petrou
AU  - Pogodin, Pavel
AU  - Poroikov, Vladimir
AU  - Ivanov, Marija
AU  - Kostić, Marina
AU  - Soković, Marina
AU  - Eleftheriou, Phaedra
PY  - 2020
UR  - https://www.mdpi.com/1424-8247/13/9/229
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3942
AB  - Herein we report the design, synthesis, computational, and experimental evaluation of the antimicrobial activity of fourteen new 3-amino-5-(indol-3-yl) methylene-4-oxo-2-thioxothiazolidine derivatives. The structures were designed, and their antimicrobial activity and toxicity were predicted in silico. All synthesized compounds exhibited antibacterial activity against eight Gram-positive and Gram-negative bacteria. Their activity exceeded those of ampicillin and (for the majority of compounds) streptomycin. The most sensitive bacterium was S. aureus (American Type Culture Collection ATCC 6538), while L. monocytogenes (NCTC 7973) was the most resistant. The best antibacterial activity was observed for compound 5d (Z)-N-(5-((1H-indol-3-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)-4-hydroxybenzamide (Minimal inhibitory concentration, MIC at 37.9–113.8 μM, and Minimal bactericidal concentration MBC at 57.8–118.3 μM). Three most active compounds 5d, 5g, and 5k being evaluated against three resistant strains, Methicillin resistant Staphilococcus aureus (MRSA), P. aeruginosa, and E. coli, were more potent against MRSA than ampicillin (MIC at 248–372 μM, MBC at 372–1240 μM). At the same time, streptomycin (MIC at 43–172 μM, MBC at 86–344 μM) did not show bactericidal activity at all. The compound 5d was also more active than ampicillin towards resistant P. aeruginosa strain. Antifungal activity of all compounds exceeded those of the reference antifungal agents bifonazole (MIC at 480–640 μM, and MFC at 640–800 μM) and ketoconazole (MIC 285–475 μM and MFC 380–950 μM). The best activity was exhibited by compound 5g. The most sensitive fungal was T. viride (IAM 5061), while A. fumigatus (human isolate) was the most resistant. Low cytotoxicity against HEK-293 human embryonic kidney cell line and reasonable selectivity indices were shown for the most active compounds 5d, 5g, 5k, 7c using thiazolyl blue tetrazolium bromide MTT assay. The docking studies indicated a probable involvement of E. coli Mur B inhibition in the antibacterial action, while CYP51 inhibition is likely responsible for the antifungal activity of the tested compounds.
PB  - MDPI AG
T2  - Pharmaceuticals
T1  - 3-Amino-5-(indol-3-yl)methylene-4-oxo-2-thioxothiazolidine Derivatives as Antimicrobial Agents: Synthesis, Computational and Biological Evaluation
IS  - 9
VL  - 13
DO  - 10.3390/ph13090229
SP  - 229
ER  - 

@article{
author = "Horishny, Volodymyr and Kartsev, Victor and Matiychuk, Vasyl and Geronikaki, Athina and Anthi, Petrou and Pogodin, Pavel and Poroikov, Vladimir and Ivanov, Marija and Kostić, Marina and Soković, Marina and Eleftheriou, Phaedra",
year = "2020",
abstract = "Herein we report the design, synthesis, computational, and experimental evaluation of the antimicrobial activity of fourteen new 3-amino-5-(indol-3-yl) methylene-4-oxo-2-thioxothiazolidine derivatives. The structures were designed, and their antimicrobial activity and toxicity were predicted in silico. All synthesized compounds exhibited antibacterial activity against eight Gram-positive and Gram-negative bacteria. Their activity exceeded those of ampicillin and (for the majority of compounds) streptomycin. The most sensitive bacterium was S. aureus (American Type Culture Collection ATCC 6538), while L. monocytogenes (NCTC 7973) was the most resistant. The best antibacterial activity was observed for compound 5d (Z)-N-(5-((1H-indol-3-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)-4-hydroxybenzamide (Minimal inhibitory concentration, MIC at 37.9–113.8 μM, and Minimal bactericidal concentration MBC at 57.8–118.3 μM). Three most active compounds 5d, 5g, and 5k being evaluated against three resistant strains, Methicillin resistant Staphilococcus aureus (MRSA), P. aeruginosa, and E. coli, were more potent against MRSA than ampicillin (MIC at 248–372 μM, MBC at 372–1240 μM). At the same time, streptomycin (MIC at 43–172 μM, MBC at 86–344 μM) did not show bactericidal activity at all. The compound 5d was also more active than ampicillin towards resistant P. aeruginosa strain. Antifungal activity of all compounds exceeded those of the reference antifungal agents bifonazole (MIC at 480–640 μM, and MFC at 640–800 μM) and ketoconazole (MIC 285–475 μM and MFC 380–950 μM). The best activity was exhibited by compound 5g. The most sensitive fungal was T. viride (IAM 5061), while A. fumigatus (human isolate) was the most resistant. Low cytotoxicity against HEK-293 human embryonic kidney cell line and reasonable selectivity indices were shown for the most active compounds 5d, 5g, 5k, 7c using thiazolyl blue tetrazolium bromide MTT assay. The docking studies indicated a probable involvement of E. coli Mur B inhibition in the antibacterial action, while CYP51 inhibition is likely responsible for the antifungal activity of the tested compounds.",
publisher = "MDPI AG",
journal = "Pharmaceuticals",
title = "3-Amino-5-(indol-3-yl)methylene-4-oxo-2-thioxothiazolidine Derivatives as Antimicrobial Agents: Synthesis, Computational and Biological Evaluation",
number = "9",
volume = "13",
doi = "10.3390/ph13090229",
pages = "229"
}

Horishny, V., Kartsev, V., Matiychuk, V., Geronikaki, A., Anthi, P., Pogodin, P., Poroikov, V., Ivanov, M., Kostić, M., Soković, M.,& Eleftheriou, P.. (2020). 3-Amino-5-(indol-3-yl)methylene-4-oxo-2-thioxothiazolidine Derivatives as Antimicrobial Agents: Synthesis, Computational and Biological Evaluation. in Pharmaceuticals
MDPI AG., 13(9), 229.
https://doi.org/10.3390/ph13090229

Horishny V, Kartsev V, Matiychuk V, Geronikaki A, Anthi P, Pogodin P, Poroikov V, Ivanov M, Kostić M, Soković M, Eleftheriou P. 3-Amino-5-(indol-3-yl)methylene-4-oxo-2-thioxothiazolidine Derivatives as Antimicrobial Agents: Synthesis, Computational and Biological Evaluation. in Pharmaceuticals. 2020;13(9):229.
doi:10.3390/ph13090229 .

Horishny, Volodymyr, Kartsev, Victor, Matiychuk, Vasyl, Geronikaki, Athina, Anthi, Petrou, Pogodin, Pavel, Poroikov, Vladimir, Ivanov, Marija, Kostić, Marina, Soković, Marina, Eleftheriou, Phaedra, "3-Amino-5-(indol-3-yl)methylene-4-oxo-2-thioxothiazolidine Derivatives as Antimicrobial Agents: Synthesis, Computational and Biological Evaluation" in Pharmaceuticals, 13, no. 9 (2020):229,
https://doi.org/10.3390/ph13090229 . .

TY  - JOUR
AU  - Horishny, Volodymyr
AU  - Kartsev, Victor
AU  - Geronikaki, Athina
AU  - Matiychuk, Vasyl
AU  - Petrou, Anthi
AU  - Glamočlija, Jasmina
AU  - Ćirić, Ana
AU  - Soković, Marina
PY  - 2020
UR  - https://www.mdpi.com/1420-3049/25/8/1964
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3661
AB  - Background: Infectious diseases symbolize a global consequential strain on public health security and impact on the socio-economic stability all over the world. The increasing resistance to the current antimicrobial treatment has resulted in crucial need for the discovery and development of novel entity for the infectious treatment with different modes of action that could target both sensitive and resistant strains. Methods: Compounds were synthesized using classical methods of organic synthesis. Results: All 20 synthesized compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species. It should be mentioned that all compounds exhibited better antibacterial potency than ampicillin against all bacteria tested. Furthermore, 18 compounds appeared to be more potent than streptomycin against Staphylococcus aureus, Enterobacter cloacae, Pseudomonas aeruginosa, Listeria monocytogenes, and Escherichia coli. Three the most active compounds 4h, 5b, and 5g appeared to be more potent against MRSA than ampicillin, while streptomycin did not show any bactericidal activity. All three compounds displayed better activity also against resistant strains P. aeruginosa and E. coli than ampicillin. Furthermore, all compounds were able to inhibit biofilm formation 2- to 4-times more than both reference drugs. Compounds were evaluated also for their antifungal activity against eight species. The evaluation revealed that all compounds exhibited antifungal activity better than the reference drugs bifonazole and ketoconazole. Molecular docking studies on antibacterial and antifungal targets were performed in order to elucidate the mechanism of antibacterial activity of synthesized compounds. Conclusion: All tested compounds showed good antibacterial and antifungal activity better than that of reference drugs and three the most active compounds could consider as lead compounds for the development of new more potent agents.
PB  - MDPI AG
T2  - Molecules
T1  - 5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl)alkancarboxylic Acids as Antimicrobial Agents: Synthesis, Biological Evaluation, and Molecular Docking Studies
IS  - 8
VL  - 25
DO  - 10.3390/molecules25081964
SP  - 1964
ER  - 

@article{
author = "Horishny, Volodymyr and Kartsev, Victor and Geronikaki, Athina and Matiychuk, Vasyl and Petrou, Anthi and Glamočlija, Jasmina and Ćirić, Ana and Soković, Marina",
year = "2020",
abstract = "Background: Infectious diseases symbolize a global consequential strain on public health security and impact on the socio-economic stability all over the world. The increasing resistance to the current antimicrobial treatment has resulted in crucial need for the discovery and development of novel entity for the infectious treatment with different modes of action that could target both sensitive and resistant strains. Methods: Compounds were synthesized using classical methods of organic synthesis. Results: All 20 synthesized compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species. It should be mentioned that all compounds exhibited better antibacterial potency than ampicillin against all bacteria tested. Furthermore, 18 compounds appeared to be more potent than streptomycin against Staphylococcus aureus, Enterobacter cloacae, Pseudomonas aeruginosa, Listeria monocytogenes, and Escherichia coli. Three the most active compounds 4h, 5b, and 5g appeared to be more potent against MRSA than ampicillin, while streptomycin did not show any bactericidal activity. All three compounds displayed better activity also against resistant strains P. aeruginosa and E. coli than ampicillin. Furthermore, all compounds were able to inhibit biofilm formation 2- to 4-times more than both reference drugs. Compounds were evaluated also for their antifungal activity against eight species. The evaluation revealed that all compounds exhibited antifungal activity better than the reference drugs bifonazole and ketoconazole. Molecular docking studies on antibacterial and antifungal targets were performed in order to elucidate the mechanism of antibacterial activity of synthesized compounds. Conclusion: All tested compounds showed good antibacterial and antifungal activity better than that of reference drugs and three the most active compounds could consider as lead compounds for the development of new more potent agents.",
publisher = "MDPI AG",
journal = "Molecules",
title = "5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl)alkancarboxylic Acids as Antimicrobial Agents: Synthesis, Biological Evaluation, and Molecular Docking Studies",
number = "8",
volume = "25",
doi = "10.3390/molecules25081964",
pages = "1964"
}

Horishny, V., Kartsev, V., Geronikaki, A., Matiychuk, V., Petrou, A., Glamočlija, J., Ćirić, A.,& Soković, M.. (2020). 5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl)alkancarboxylic Acids as Antimicrobial Agents: Synthesis, Biological Evaluation, and Molecular Docking Studies. in Molecules
MDPI AG., 25(8), 1964.
https://doi.org/10.3390/molecules25081964

Horishny V, Kartsev V, Geronikaki A, Matiychuk V, Petrou A, Glamočlija J, Ćirić A, Soković M. 5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl)alkancarboxylic Acids as Antimicrobial Agents: Synthesis, Biological Evaluation, and Molecular Docking Studies. in Molecules. 2020;25(8):1964.
doi:10.3390/molecules25081964 .

Horishny, Volodymyr, Kartsev, Victor, Geronikaki, Athina, Matiychuk, Vasyl, Petrou, Anthi, Glamočlija, Jasmina, Ćirić, Ana, Soković, Marina, "5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxothiazolidin-3-yl)alkancarboxylic Acids as Antimicrobial Agents: Synthesis, Biological Evaluation, and Molecular Docking Studies" in Molecules, 25, no. 8 (2020):1964,
https://doi.org/10.3390/molecules25081964 . .

TY  - JOUR
AU  - Kartsev, Victor
AU  - Lichitsky, Boris
AU  - Geronikaki, Athina
AU  - Petrou, Anthi
AU  - Ivanov, Marija
AU  - Kostić, Marina
AU  - Radanović, Oliver
AU  - Soković, Marina
PY  - 2019
UR  - http://xlink.rsc.org/?DOI=C8MD90056F
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3252
AB  - The authors regret that the author names were not displayed correctly on the original manuscript. The corrected list of authors for this paper is as shown above. The Royal Society of Chemistry apologises for these errors and any consequent inconvenience to authors and readers.
T2  - MedChemComm
T2  - MedChemComm
T1  - Correction: Design, synthesis and antimicrobial activity of usnic acid derivatives (MedChemComm (2018) 9 (870–882) DOI: 10.1039/C8MD00076J)
IS  - 1
VL  - 10
DO  - 10.1039/C8MD90056F
SP  - 180
ER  - 

@article{
author = "Kartsev, Victor and Lichitsky, Boris and Geronikaki, Athina and Petrou, Anthi and Ivanov, Marija and Kostić, Marina and Radanović, Oliver and Soković, Marina",
year = "2019",
abstract = "The authors regret that the author names were not displayed correctly on the original manuscript. The corrected list of authors for this paper is as shown above. The Royal Society of Chemistry apologises for these errors and any consequent inconvenience to authors and readers.",
journal = "MedChemComm, MedChemComm",
title = "Correction: Design, synthesis and antimicrobial activity of usnic acid derivatives (MedChemComm (2018) 9 (870–882) DOI: 10.1039/C8MD00076J)",
number = "1",
volume = "10",
doi = "10.1039/C8MD90056F",
pages = "180"
}

Kartsev, V., Lichitsky, B., Geronikaki, A., Petrou, A., Ivanov, M., Kostić, M., Radanović, O.,& Soković, M.. (2019). Correction: Design, synthesis and antimicrobial activity of usnic acid derivatives (MedChemComm (2018) 9 (870–882) DOI: 10.1039/C8MD00076J). in MedChemComm, 10(1), 180.
https://doi.org/10.1039/C8MD90056F

Kartsev V, Lichitsky B, Geronikaki A, Petrou A, Ivanov M, Kostić M, Radanović O, Soković M. Correction: Design, synthesis and antimicrobial activity of usnic acid derivatives (MedChemComm (2018) 9 (870–882) DOI: 10.1039/C8MD00076J). in MedChemComm. 2019;10(1):180.
doi:10.1039/C8MD90056F .

Kartsev, Victor, Lichitsky, Boris, Geronikaki, Athina, Petrou, Anthi, Ivanov, Marija, Kostić, Marina, Radanović, Oliver, Soković, Marina, "Correction: Design, synthesis and antimicrobial activity of usnic acid derivatives (MedChemComm (2018) 9 (870–882) DOI: 10.1039/C8MD00076J)" in MedChemComm, 10, no. 1 (2019):180,
https://doi.org/10.1039/C8MD90056F . .

TY  - JOUR
AU  - Kartsev, Victor
AU  - Geronikaki, Athina
AU  - Petrou, Anthi
AU  - Lichitsky, Boris
AU  - Kostić, Marina
AU  - Ivanov, Marija
AU  - Soković, Marina
AU  - Sirakanyan, Samvel
PY  - 2019
UR  - http://www.eurekaselect.com/172243/article
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3469
AB  - BACKGROUND Griseofulvin - a mold metabolite produced by Penisilium griseofulvum is known as an antifungal drug. OBJECTIVE Thus, the goal of this paper is the design and synthesis of new griseofulvin derivatives and evaluation of their antifungal activity. METHODS Forty-two new compounds were synthesized using classical methods of organic synthesis and evaluated for their antimicrobial activity by microdilution method. RESULTS All forty-two new compounds exhibited very good activity against eight tested micromycetes with MIC ranging from 0.0075-0.055 mg/ml and MFC from 0.02-024 mg/ml. All compounds exhibited better activity than reference drugs ketoconazole (7-42 times) and bifonazole (3-16 fold). The most promising was compound 15. The most sensitive fungal was found to be T. viride, while the most resistant, as was expected, was A. fumigatus. It should be mentioned that most of compounds exhibited better activity than griseofulvin. The molecular docking studies revealed that the most active compound have the same hydrophobic and H-bonding interactions with Thr276 residue observed for griseofulvin forming 3 hydrogen bonds while griseofulvin only one. In general, the molecular docking results coincide with experimental. CONCLUSION Forty-two giseofulvin derivatives were designed, synthesized and evaluated for antimicrobial activity. These derivatives revealed good antifungal activity, better than reference drugs ketoconazole, bifonazole, and griseofulvin as well.
T2  - Current Topics in Medicinal Chemistry
T1  - Griseofulvin Derivatives: Synthesis, Molecular Docking and Biological Evaluation.
IS  - 13
VL  - 19
DO  - 10.2174/1568026619666190523080136
SP  - 1145
EP  - 1161
ER  - 

@article{
author = "Kartsev, Victor and Geronikaki, Athina and Petrou, Anthi and Lichitsky, Boris and Kostić, Marina and Ivanov, Marija and Soković, Marina and Sirakanyan, Samvel",
year = "2019",
abstract = "BACKGROUND Griseofulvin - a mold metabolite produced by Penisilium griseofulvum is known as an antifungal drug. OBJECTIVE Thus, the goal of this paper is the design and synthesis of new griseofulvin derivatives and evaluation of their antifungal activity. METHODS Forty-two new compounds were synthesized using classical methods of organic synthesis and evaluated for their antimicrobial activity by microdilution method. RESULTS All forty-two new compounds exhibited very good activity against eight tested micromycetes with MIC ranging from 0.0075-0.055 mg/ml and MFC from 0.02-024 mg/ml. All compounds exhibited better activity than reference drugs ketoconazole (7-42 times) and bifonazole (3-16 fold). The most promising was compound 15. The most sensitive fungal was found to be T. viride, while the most resistant, as was expected, was A. fumigatus. It should be mentioned that most of compounds exhibited better activity than griseofulvin. The molecular docking studies revealed that the most active compound have the same hydrophobic and H-bonding interactions with Thr276 residue observed for griseofulvin forming 3 hydrogen bonds while griseofulvin only one. In general, the molecular docking results coincide with experimental. CONCLUSION Forty-two giseofulvin derivatives were designed, synthesized and evaluated for antimicrobial activity. These derivatives revealed good antifungal activity, better than reference drugs ketoconazole, bifonazole, and griseofulvin as well.",
journal = "Current Topics in Medicinal Chemistry",
title = "Griseofulvin Derivatives: Synthesis, Molecular Docking and Biological Evaluation.",
number = "13",
volume = "19",
doi = "10.2174/1568026619666190523080136",
pages = "1145-1161"
}

Kartsev, V., Geronikaki, A., Petrou, A., Lichitsky, B., Kostić, M., Ivanov, M., Soković, M.,& Sirakanyan, S.. (2019). Griseofulvin Derivatives: Synthesis, Molecular Docking and Biological Evaluation.. in Current Topics in Medicinal Chemistry, 19(13), 1145-1161.
https://doi.org/10.2174/1568026619666190523080136

Kartsev V, Geronikaki A, Petrou A, Lichitsky B, Kostić M, Ivanov M, Soković M, Sirakanyan S. Griseofulvin Derivatives: Synthesis, Molecular Docking and Biological Evaluation.. in Current Topics in Medicinal Chemistry. 2019;19(13):1145-1161.
doi:10.2174/1568026619666190523080136 .

Kartsev, Victor, Geronikaki, Athina, Petrou, Anthi, Lichitsky, Boris, Kostić, Marina, Ivanov, Marija, Soković, Marina, Sirakanyan, Samvel, "Griseofulvin Derivatives: Synthesis, Molecular Docking and Biological Evaluation." in Current Topics in Medicinal Chemistry, 19, no. 13 (2019):1145-1161,
https://doi.org/10.2174/1568026619666190523080136 . .

TY  - JOUR
AU  - Kartsev, Victor
AU  - Lichitsky, Boris
AU  - Geronikaki, Athina
AU  - Petrou, Anthi
AU  - Ivanov, Marija
AU  - Kostić, Marina
AU  - Radanović, Oliver
AU  - Soković, Marina
PY  - 2018
UR  - http://pubs.rsc.org/en/Content/ArticleLanding/2018/MD/C8MD00076J#!divAbstract
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3080
AB  - Usnic acid, a dibenzofuran, was originally isolated from lichens producing secondary metabolites, and is well known as an antibiotic, but is also endowed with several other interesting properties. Thus, the goal of this paper is the design of new usnic acid derivatives and evaluation of their antimicrobial activity. All newly synthesized compounds possess good antibacterial activity with MIC ranging from 1.02-50.93 × 10-2 mmol mL-1 and MBC from 2.05-70.57 × 10-2 mmol mL-1. The most sensitive bacterial species was Staphylococcus aureus, while Pseudomonas aeruginosa and Escherichia coli were the most resistant among the ATCC strains, and MRSA was the most resistant among all tested bacteria (ATCC and clinical isolates). Their antifungal activity was very strong (MIC = 0.35-7.53 × 10-2 mmol mL-1 and MFC = 0.70-15.05 × 10-2 mmol mL-1)-better than those of reference compounds and usnic acid itself. The most sensitive fungal species was Trichoderma viride, while Penicillium versicolor var. cyclopium appeared to be the most resistant. It should be mentioned that in general most of the compounds showed weaker antibacterial activity, but better antifungal properties than usnic acid itself. The results allow us to conclude that the title compounds are good lead compounds for novel more active antibacterial drugs. On the other hand, these compounds are very promising as antifungals.
T2  - MedChemComm
T2  - MedChemComm
T1  - Design, synthesis and antimicrobial activity of usnic acid derivatives
IS  - 5
VL  - 9
DO  - 10.1039/C8MD00076J
SP  - 870
EP  - 882
ER  - 

@article{
author = "Kartsev, Victor and Lichitsky, Boris and Geronikaki, Athina and Petrou, Anthi and Ivanov, Marija and Kostić, Marina and Radanović, Oliver and Soković, Marina",
year = "2018",
abstract = "Usnic acid, a dibenzofuran, was originally isolated from lichens producing secondary metabolites, and is well known as an antibiotic, but is also endowed with several other interesting properties. Thus, the goal of this paper is the design of new usnic acid derivatives and evaluation of their antimicrobial activity. All newly synthesized compounds possess good antibacterial activity with MIC ranging from 1.02-50.93 × 10-2 mmol mL-1 and MBC from 2.05-70.57 × 10-2 mmol mL-1. The most sensitive bacterial species was Staphylococcus aureus, while Pseudomonas aeruginosa and Escherichia coli were the most resistant among the ATCC strains, and MRSA was the most resistant among all tested bacteria (ATCC and clinical isolates). Their antifungal activity was very strong (MIC = 0.35-7.53 × 10-2 mmol mL-1 and MFC = 0.70-15.05 × 10-2 mmol mL-1)-better than those of reference compounds and usnic acid itself. The most sensitive fungal species was Trichoderma viride, while Penicillium versicolor var. cyclopium appeared to be the most resistant. It should be mentioned that in general most of the compounds showed weaker antibacterial activity, but better antifungal properties than usnic acid itself. The results allow us to conclude that the title compounds are good lead compounds for novel more active antibacterial drugs. On the other hand, these compounds are very promising as antifungals.",
journal = "MedChemComm, MedChemComm",
title = "Design, synthesis and antimicrobial activity of usnic acid derivatives",
number = "5",
volume = "9",
doi = "10.1039/C8MD00076J",
pages = "870-882"
}

Kartsev, V., Lichitsky, B., Geronikaki, A., Petrou, A., Ivanov, M., Kostić, M., Radanović, O.,& Soković, M.. (2018). Design, synthesis and antimicrobial activity of usnic acid derivatives. in MedChemComm, 9(5), 870-882.
https://doi.org/10.1039/C8MD00076J

Kartsev V, Lichitsky B, Geronikaki A, Petrou A, Ivanov M, Kostić M, Radanović O, Soković M. Design, synthesis and antimicrobial activity of usnic acid derivatives. in MedChemComm. 2018;9(5):870-882.
doi:10.1039/C8MD00076J .

Kartsev, Victor, Lichitsky, Boris, Geronikaki, Athina, Petrou, Anthi, Ivanov, Marija, Kostić, Marina, Radanović, Oliver, Soković, Marina, "Design, synthesis and antimicrobial activity of usnic acid derivatives" in MedChemComm, 9, no. 5 (2018):870-882,
https://doi.org/10.1039/C8MD00076J . .