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  - 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 . .