TY  - JOUR
AU  - Tratrat, Christophe
AU  - Petrou, Anthi
AU  - Geronikaki, Athina
AU  - Ivanov, Marija
AU  - Kostić, Marina
AU  - Soković, Marina
AU  - Vizirianakis, Ioannis S.
AU  - Theodoroula, Nikoleta F.
AU  - Haroun, Michelyne
PY  - 2022
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/4936
AB  - Herein, we report computational and experimental evaluations of the antimicrobial activity of twenty one 2,3-diaryl-thiazolidin-4-ones. All synthesized compounds exhibited an antibacterial activity against six Gram-positive and Gram-negative bacteria to different extents. Thus, the MIC was in the range of 0.008–0.24 mg/mL, while the MBC was 0.0016–0.48 mg/mL. The most sensitive bacterium was S. Typhimurium, whereas S. aureus was the most resistant. The best antibacterial activity was observed for compound 5 (MIC at 0.008–0.06 mg/mL). The three most active compounds 5, 8, and 15, as well as compound 6, which were evaluated against three resistant strains, MRSA, P. aeruginosa, and E. coli, were more potent against all bacterial strains used than ampicillin. The antifungal activity of some compounds exceeded or were equipotent with those of the reference antifungal agents bifonazole and ketoconazole. The best activity was expressed by compound 5. All compounds exhibited moderate to good drug-likeness scores ranging from −0.39 to 0.39. 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. Finally, the assessment of cellular cytotoxicity of the compounds in normal human MRC-5 cells revealed that the compounds were not toxic. View Full-Text
PB  - Basel: MDPI
T2  - Molecules
T1  - Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation
IS  - 6
VL  - 27
DO  - 10.3390/molecules27061930
SP  - 1930
ER  - 

@article{
author = "Tratrat, Christophe and Petrou, Anthi and Geronikaki, Athina and Ivanov, Marija and Kostić, Marina and Soković, Marina and Vizirianakis, Ioannis S. and Theodoroula, Nikoleta F. and Haroun, Michelyne",
year = "2022",
abstract = "Herein, we report computational and experimental evaluations of the antimicrobial activity of twenty one 2,3-diaryl-thiazolidin-4-ones. All synthesized compounds exhibited an antibacterial activity against six Gram-positive and Gram-negative bacteria to different extents. Thus, the MIC was in the range of 0.008–0.24 mg/mL, while the MBC was 0.0016–0.48 mg/mL. The most sensitive bacterium was S. Typhimurium, whereas S. aureus was the most resistant. The best antibacterial activity was observed for compound 5 (MIC at 0.008–0.06 mg/mL). The three most active compounds 5, 8, and 15, as well as compound 6, which were evaluated against three resistant strains, MRSA, P. aeruginosa, and E. coli, were more potent against all bacterial strains used than ampicillin. The antifungal activity of some compounds exceeded or were equipotent with those of the reference antifungal agents bifonazole and ketoconazole. The best activity was expressed by compound 5. All compounds exhibited moderate to good drug-likeness scores ranging from −0.39 to 0.39. 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. Finally, the assessment of cellular cytotoxicity of the compounds in normal human MRC-5 cells revealed that the compounds were not toxic. View Full-Text",
publisher = "Basel: MDPI",
journal = "Molecules",
title = "Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation",
number = "6",
volume = "27",
doi = "10.3390/molecules27061930",
pages = "1930"
}

Tratrat, C., Petrou, A., Geronikaki, A., Ivanov, M., Kostić, M., Soković, M., Vizirianakis, I. S., Theodoroula, N. F.,& Haroun, M.. (2022). Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation. in Molecules
Basel: MDPI., 27(6), 1930.
https://doi.org/10.3390/molecules27061930

Tratrat C, Petrou A, Geronikaki A, Ivanov M, Kostić M, Soković M, Vizirianakis IS, Theodoroula NF, Haroun M. Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation. in Molecules. 2022;27(6):1930.
doi:10.3390/molecules27061930 .

Tratrat, Christophe, Petrou, Anthi, Geronikaki, Athina, Ivanov, Marija, Kostić, Marina, Soković, Marina, Vizirianakis, Ioannis S., Theodoroula, Nikoleta F., Haroun, Michelyne, "Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation" in Molecules, 27, no. 6 (2022):1930,
https://doi.org/10.3390/molecules27061930 . .

TY  - JOUR
AU  - Haroun, Michelyne
AU  - Tratrat, Christophe
AU  - Petrou, Anthi
AU  - Geronikaki, Athina
AU  - Ivanov, Marija
AU  - Ćirić, Ana
AU  - Soković, Marina
PY  - 2021
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/4300
AB  - The search for new antimicrobial agents is greater than ever due to the perpetual threat of multidrug resistance in known pathogens and the relentless emergence of new infections. In this manuscript, ten thiazole-based thiazolidinone hybrids bearing a 6-trifluoromethoxy substituent on the benzothiazole core were synthesized and evaluated against a panel of four bacterial strains Salmonella typhimurium, Staphylococcus aureus, Escherichia coli and Listeria monocytogenes and three resistant strains Pseudomonas aeruginosa, E. coli and MRSA. The evaluation of minimum bactericidal and minimum inhibitory concentrations was accomplished by microdilution assay. As reference compounds ampicillin and streptomycin were employed. All compounds displayed antibacterial efficiencies with MBCs/MICs at 0.25-1 mg/mL and 0.12-1 mg/mL respectively while ampicillin displayed MBCs/MICs at 0.15-0.3 mg/mL and at 0.1-0.2 mg/mL respectively. MICs/MBC of streptomycin varied from 0.05 to 0.15 mg/mL and from 0.1 to 0.3 mg/mL respectively. The best overall effect was observed for compound h4, while compound h1 exhibited the highest effective action against E. coli (MIC/MBC 0.12/0.25 mg/ml) among all tested compounds.
PB  - Elsevier
T2  - Bioorganic & Medicinal Chemistry Letters
T1  - 2-Aryl-3-(6-trifluoromethoxy)benzo[d]thiazole-based thiazolidinone hybrids as potential anti-infective agents: Synthesis, biological evaluation and molecular docking studies
IS  - 15
VL  - 32
DO  - 10.1016/j.bmcl.2020.127718
SP  - 127718
ER  - 

@article{
author = "Haroun, Michelyne and Tratrat, Christophe and Petrou, Anthi and Geronikaki, Athina and Ivanov, Marija and Ćirić, Ana and Soković, Marina",
year = "2021",
abstract = "The search for new antimicrobial agents is greater than ever due to the perpetual threat of multidrug resistance in known pathogens and the relentless emergence of new infections. In this manuscript, ten thiazole-based thiazolidinone hybrids bearing a 6-trifluoromethoxy substituent on the benzothiazole core were synthesized and evaluated against a panel of four bacterial strains Salmonella typhimurium, Staphylococcus aureus, Escherichia coli and Listeria monocytogenes and three resistant strains Pseudomonas aeruginosa, E. coli and MRSA. The evaluation of minimum bactericidal and minimum inhibitory concentrations was accomplished by microdilution assay. As reference compounds ampicillin and streptomycin were employed. All compounds displayed antibacterial efficiencies with MBCs/MICs at 0.25-1 mg/mL and 0.12-1 mg/mL respectively while ampicillin displayed MBCs/MICs at 0.15-0.3 mg/mL and at 0.1-0.2 mg/mL respectively. MICs/MBC of streptomycin varied from 0.05 to 0.15 mg/mL and from 0.1 to 0.3 mg/mL respectively. The best overall effect was observed for compound h4, while compound h1 exhibited the highest effective action against E. coli (MIC/MBC 0.12/0.25 mg/ml) among all tested compounds.",
publisher = "Elsevier",
journal = "Bioorganic & Medicinal Chemistry Letters",
title = "2-Aryl-3-(6-trifluoromethoxy)benzo[d]thiazole-based thiazolidinone hybrids as potential anti-infective agents: Synthesis, biological evaluation and molecular docking studies",
number = "15",
volume = "32",
doi = "10.1016/j.bmcl.2020.127718",
pages = "127718"
}

Haroun, M., Tratrat, C., Petrou, A., Geronikaki, A., Ivanov, M., Ćirić, A.,& Soković, M.. (2021). 2-Aryl-3-(6-trifluoromethoxy)benzo[d]thiazole-based thiazolidinone hybrids as potential anti-infective agents: Synthesis, biological evaluation and molecular docking studies. in Bioorganic & Medicinal Chemistry Letters
Elsevier., 32(15), 127718.
https://doi.org/10.1016/j.bmcl.2020.127718

Haroun M, Tratrat C, Petrou A, Geronikaki A, Ivanov M, Ćirić A, Soković M. 2-Aryl-3-(6-trifluoromethoxy)benzo[d]thiazole-based thiazolidinone hybrids as potential anti-infective agents: Synthesis, biological evaluation and molecular docking studies. in Bioorganic & Medicinal Chemistry Letters. 2021;32(15):127718.
doi:10.1016/j.bmcl.2020.127718 .

Haroun, Michelyne, Tratrat, Christophe, Petrou, Anthi, Geronikaki, Athina, Ivanov, Marija, Ćirić, Ana, Soković, Marina, "2-Aryl-3-(6-trifluoromethoxy)benzo[d]thiazole-based thiazolidinone hybrids as potential anti-infective agents: Synthesis, biological evaluation and molecular docking studies" in Bioorganic & Medicinal Chemistry Letters, 32, no. 15 (2021):127718,
https://doi.org/10.1016/j.bmcl.2020.127718 . .

TY  - JOUR
AU  - Haroun, Michelyne
AU  - Tratrat, Christophe
AU  - Kolokotroni, Aggeliki
AU  - Petrou, Anthi
AU  - Geronikaki, Athina
AU  - Ivanov, Marija
AU  - Kostić, Marina
AU  - Soković, Marina
AU  - Carazo, Alejandro
AU  - Mladěnka, Přemysl
AU  - Sreeharsha, Nagaraja
AU  - Venugopala, Katharigatta N.
AU  - Nair, Anroop B.
AU  - Elsewedy, Heba S.
PY  - 2021
UR  - https://www.mdpi.com/2079-6382/10/3/309
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/4196
AB  - In this study, we report the design, synthesis, computational and experimental evaluation of the antimicrobial activity, as well as docking studies of new 5-methylthiazole based thiazolidinones. All compounds demonstrated antibacterial efficacy, some of which (1, 4, 10 and 13) exhibited good activity against E. coli and B. cereus. The evaluation of antibacterial activity against three resistant strains, MRSA, P. aeruginosa and E. coli, revealed that compound 12 showed the best activity, higher than reference drugs ampicillin and streptomycin, which were inactive or exhibited only bacteriostatic activity against MRSA, respectively. Ten out of fifteen compounds demonstrated higher potency than reference drugs against a resistant strain of E. coli, which appeared to be the most sensitive species to our compounds. Compounds 8, 13 and 14 applied in a concentration equal to MIC reduced P. aeruginosa biofilm formation by more than 50%. All compounds displayed antifungal activity, with compound 10 being the most active. The majority of compounds showed better activity than ketoconazole against almost all fungal strains. In order to elucidate the mechanism of antibacterial and antifungal activities, molecular docking studies on E. coli Mur B and C. albicans CYP51 and dihydrofolate reductase were performed. Docking analysis of E. coli MurB indicated a probable involvement of MurB inhibition in the antibacterial mechanism of tested compounds while docking to 14α-lanosterol demethylase (CYP51) and tetrahydrofolate reductase of Candida albicans suggested that probable involvement of inhibition of CYP51 reductase in the antifungal activity of the compounds. Potential toxicity toward human cells is also reported.
PB  - MDPI AG
T2  - Antibiotics
T1  - 5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies
IS  - 3
VL  - 10
DO  - 10.3390/antibiotics10030309
SP  - 309
ER  - 

@article{
author = "Haroun, Michelyne and Tratrat, Christophe and Kolokotroni, Aggeliki and Petrou, Anthi and Geronikaki, Athina and Ivanov, Marija and Kostić, Marina and Soković, Marina and Carazo, Alejandro and Mladěnka, Přemysl and Sreeharsha, Nagaraja and Venugopala, Katharigatta N. and Nair, Anroop B. and Elsewedy, Heba S.",
year = "2021",
abstract = "In this study, we report the design, synthesis, computational and experimental evaluation of the antimicrobial activity, as well as docking studies of new 5-methylthiazole based thiazolidinones. All compounds demonstrated antibacterial efficacy, some of which (1, 4, 10 and 13) exhibited good activity against E. coli and B. cereus. The evaluation of antibacterial activity against three resistant strains, MRSA, P. aeruginosa and E. coli, revealed that compound 12 showed the best activity, higher than reference drugs ampicillin and streptomycin, which were inactive or exhibited only bacteriostatic activity against MRSA, respectively. Ten out of fifteen compounds demonstrated higher potency than reference drugs against a resistant strain of E. coli, which appeared to be the most sensitive species to our compounds. Compounds 8, 13 and 14 applied in a concentration equal to MIC reduced P. aeruginosa biofilm formation by more than 50%. All compounds displayed antifungal activity, with compound 10 being the most active. The majority of compounds showed better activity than ketoconazole against almost all fungal strains. In order to elucidate the mechanism of antibacterial and antifungal activities, molecular docking studies on E. coli Mur B and C. albicans CYP51 and dihydrofolate reductase were performed. Docking analysis of E. coli MurB indicated a probable involvement of MurB inhibition in the antibacterial mechanism of tested compounds while docking to 14α-lanosterol demethylase (CYP51) and tetrahydrofolate reductase of Candida albicans suggested that probable involvement of inhibition of CYP51 reductase in the antifungal activity of the compounds. Potential toxicity toward human cells is also reported.",
publisher = "MDPI AG",
journal = "Antibiotics",
title = "5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies",
number = "3",
volume = "10",
doi = "10.3390/antibiotics10030309",
pages = "309"
}

Haroun, M., Tratrat, C., Kolokotroni, A., Petrou, A., Geronikaki, A., Ivanov, M., Kostić, M., Soković, M., Carazo, A., Mladěnka, P., Sreeharsha, N., Venugopala, K. N., Nair, A. B.,& Elsewedy, H. S.. (2021). 5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies. in Antibiotics
MDPI AG., 10(3), 309.
https://doi.org/10.3390/antibiotics10030309

Haroun M, Tratrat C, Kolokotroni A, Petrou A, Geronikaki A, Ivanov M, Kostić M, Soković M, Carazo A, Mladěnka P, Sreeharsha N, Venugopala KN, Nair AB, Elsewedy HS. 5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies. in Antibiotics. 2021;10(3):309.
doi:10.3390/antibiotics10030309 .

Haroun, Michelyne, Tratrat, Christophe, Kolokotroni, Aggeliki, Petrou, Anthi, Geronikaki, Athina, Ivanov, Marija, Kostić, Marina, Soković, Marina, Carazo, Alejandro, Mladěnka, Přemysl, Sreeharsha, Nagaraja, Venugopala, Katharigatta N., Nair, Anroop B., Elsewedy, Heba S., "5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies" in Antibiotics, 10, no. 3 (2021):309,
https://doi.org/10.3390/antibiotics10030309 . .

TY  - JOUR
AU  - Haroun, Michelyne
AU  - Tratrat, Christophe
AU  - Petrou, Anthi
AU  - Geronikaki, Athina
AU  - Ivanov, Marija
AU  - Ćirić, Ana
AU  - Soković, Marina
AU  - Nagaraja, Sreeharsha
AU  - Narayanaswamy Venugopala, Katharigatta
AU  - Balachandran Nair, Anroop
AU  - Elsewedy, Heba
AU  - Kochkar, Hafedh
PY  - 2021
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/4299
AB  - Background: Infectious diseases still affect large populations causing significant morbidity
and mortality. Bacterial and fungal infections for centuries were the main factors of death and
disability of millions of humans. Despite the progress in the control of infectious diseases, the
appearance of resistance of microbes to existing drugs creates the need for the development of new
effective antimicrobial agents. In an attempt to improve the antibacterial activity of previously
synthesized compounds modifications to their structures were performed. Methods: Nineteen
thiazolidinone derivatives with 6-Cl, 4-OMe, 6-CN, 6-adamantan, 4-Me, 6-adamantan substituents at
benzothiazole ring were synthesized and evaluated against panel of four bacterial strains S. aureus,
L. monocytogenes, E. coli and S. typhimirium and three resistant strains MRSA, E. coli and P. aeruginosa
in order to improve activity of previously evaluated 6-OCF3
-benzothiazole-based thiazolidinones.
The evaluation of minimum inhibitory and minimum bactericidal concentration was determined by
microdilution method. As reference compounds ampicillin and streptomycin were used. Results:
All compounds showed antibacterial activity with MIC in range of 0.12–0.75 mg/mL and MBC at
0.25–>1.00 mg/mL The most active compound among all tested appeared to be compound 18, with
MIC at 0.10 mg/mL and MBC at 0.12 mg/mL against P. aeruginosa. as well as against resistant strain
P. aeruginosa with MIC at 0.06 mg/mL and MBC at 0.12 mg/mL almost equipotent with streptomycin
and better than ampicillin. Docking studies predicted that the inhibition of LD-carboxypeptidase is
probably the possible mechanism of antibacterial activity of tested compounds. Conclusion: The best
improvement of antibacterial activity after modifications was achieved by replacement of 6-OCF3
substituent in benzothiazole moiety by 6-Cl against S. aureus, MRSA and resistant strain of E. coli by
2.5 folds, while against L. monocytogenes and S. typhimirium from 4 to 5 folds.
PB  - MDPI
T2  - Molecules
T1  - Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation
IS  - 13
VL  - 26
DO  - 10.3390/molecules26134061
SP  - 4061
ER  - 

@article{
author = "Haroun, Michelyne and Tratrat, Christophe and Petrou, Anthi and Geronikaki, Athina and Ivanov, Marija and Ćirić, Ana and Soković, Marina and Nagaraja, Sreeharsha and Narayanaswamy Venugopala, Katharigatta and Balachandran Nair, Anroop and Elsewedy, Heba and Kochkar, Hafedh",
year = "2021",
abstract = "Background: Infectious diseases still affect large populations causing significant morbidity
and mortality. Bacterial and fungal infections for centuries were the main factors of death and
disability of millions of humans. Despite the progress in the control of infectious diseases, the
appearance of resistance of microbes to existing drugs creates the need for the development of new
effective antimicrobial agents. In an attempt to improve the antibacterial activity of previously
synthesized compounds modifications to their structures were performed. Methods: Nineteen
thiazolidinone derivatives with 6-Cl, 4-OMe, 6-CN, 6-adamantan, 4-Me, 6-adamantan substituents at
benzothiazole ring were synthesized and evaluated against panel of four bacterial strains S. aureus,
L. monocytogenes, E. coli and S. typhimirium and three resistant strains MRSA, E. coli and P. aeruginosa
in order to improve activity of previously evaluated 6-OCF3
-benzothiazole-based thiazolidinones.
The evaluation of minimum inhibitory and minimum bactericidal concentration was determined by
microdilution method. As reference compounds ampicillin and streptomycin were used. Results:
All compounds showed antibacterial activity with MIC in range of 0.12–0.75 mg/mL and MBC at
0.25–>1.00 mg/mL The most active compound among all tested appeared to be compound 18, with
MIC at 0.10 mg/mL and MBC at 0.12 mg/mL against P. aeruginosa. as well as against resistant strain
P. aeruginosa with MIC at 0.06 mg/mL and MBC at 0.12 mg/mL almost equipotent with streptomycin
and better than ampicillin. Docking studies predicted that the inhibition of LD-carboxypeptidase is
probably the possible mechanism of antibacterial activity of tested compounds. Conclusion: The best
improvement of antibacterial activity after modifications was achieved by replacement of 6-OCF3
substituent in benzothiazole moiety by 6-Cl against S. aureus, MRSA and resistant strain of E. coli by
2.5 folds, while against L. monocytogenes and S. typhimirium from 4 to 5 folds.",
publisher = "MDPI",
journal = "Molecules",
title = "Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation",
number = "13",
volume = "26",
doi = "10.3390/molecules26134061",
pages = "4061"
}

Haroun, M., Tratrat, C., Petrou, A., Geronikaki, A., Ivanov, M., Ćirić, A., Soković, M., Nagaraja, S., Narayanaswamy Venugopala, K., Balachandran Nair, A., Elsewedy, H.,& Kochkar, H.. (2021). Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation. in Molecules
MDPI., 26(13), 4061.
https://doi.org/10.3390/molecules26134061

Haroun M, Tratrat C, Petrou A, Geronikaki A, Ivanov M, Ćirić A, Soković M, Nagaraja S, Narayanaswamy Venugopala K, Balachandran Nair A, Elsewedy H, Kochkar H. Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation. in Molecules. 2021;26(13):4061.
doi:10.3390/molecules26134061 .

Haroun, Michelyne, Tratrat, Christophe, Petrou, Anthi, Geronikaki, Athina, Ivanov, Marija, Ćirić, Ana, Soković, Marina, Nagaraja, Sreeharsha, Narayanaswamy Venugopala, Katharigatta, Balachandran Nair, Anroop, Elsewedy, Heba, Kochkar, Hafedh, "Exploration of the Antimicrobial Effects of Benzothiazolylthiazolidin-4-One and In Silico Mechanistic Investigation" in Molecules, 26, no. 13 (2021):4061,
https://doi.org/10.3390/molecules26134061 . .

TY  - JOUR
AU  - Tratrat, Christophe
AU  - Haroun, Michelyne
AU  - Xenikakis, Iakovos
AU  - Liaras, Konstantinos
AU  - Tsolaki, Evangelia
AU  - Eleftheriou, Phaedra
AU  - Petrou, Anthi
AU  - Aldhubiab, Bandar
AU  - Attimarad, Mahesh
AU  - Venugopala, Katharigatta N.
AU  - Harsha, Sree
AU  - Elsewedy, Heba S.
AU  - Geronikaki, Athina
AU  - Soković, Marina
PY  - 2019
UR  - http://www.eurekaselect.com/169442/article
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3358
AB  - BACKGROUND Thiazole derivates as well as chalcones, are very important scaffold for medicinal chemistry. Literature survey revealed that they possess wide spectrum of biological activities among which are anti-inflammatory and antimicrobial. OBJECTIVES The current studies describe the synthesis and evaluation of antimicrobial activity of twenty eight novel thiazole-based chalcones. METHODS The designed compounds were synthesized using classical methods of organic synthesis. The in vivo evaluation of antimicrobial activity was performed by microdilution method. RESULTS All compounds have shown antibacterial properties better than that of ampicillin and in many cases better than streptomycin. As far as the antifungal activity is concerned, all compounds possess much higher activity than reference drugs bifonazole and ketoconazole. The most sensitive bacterial species was B. cereus (MIC 6.5-28.4 µmol × 10-2/mL and MBC 14.2-105.0 µmol × 10-2/mL) while the most resistant ones were L. monocytogenes (MIC 21.4-113.6 µmol × 10-2/mL) and E. coli (MIC 10.7- 113.6 µmol × 10-2/mL) and MBC at 42.7-358.6 µmol × 10-2/mL and 21.4-247.2 µmol × 10-2/mL, respectively. All the compounds exhibited antibacterial activity against the three resistant strains, MRSA, P. aeruginosa and E.coli. with MIC and MBC in the range of 0.65-11.00 µmol/mL × 10-2 and 1.30-16.50 µmol/mL × 10-2. Docking studies were performed. CONCLUSION Twenty-eight novel thiazole-based chalcones were designed, synthesized and evaluated for antimicrobial activity. The results showed that these derivatives could be lead compounds in search of new potent antimicrobial agents. Docking studies indicated that DNA gyrase, GyrB and MurA inhibition may explain the antibacterial activity.
T2  - Current Topics in Medicinal Chemistry
T1  - Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones.
IS  - 5
VL  - 19
DO  - 10.2174/1568026619666190129121933
SP  - 356
EP  - 375
ER  - 

@article{
author = "Tratrat, Christophe and Haroun, Michelyne and Xenikakis, Iakovos and Liaras, Konstantinos and Tsolaki, Evangelia and Eleftheriou, Phaedra and Petrou, Anthi and Aldhubiab, Bandar and Attimarad, Mahesh and Venugopala, Katharigatta N. and Harsha, Sree and Elsewedy, Heba S. and Geronikaki, Athina and Soković, Marina",
year = "2019",
abstract = "BACKGROUND Thiazole derivates as well as chalcones, are very important scaffold for medicinal chemistry. Literature survey revealed that they possess wide spectrum of biological activities among which are anti-inflammatory and antimicrobial. OBJECTIVES The current studies describe the synthesis and evaluation of antimicrobial activity of twenty eight novel thiazole-based chalcones. METHODS The designed compounds were synthesized using classical methods of organic synthesis. The in vivo evaluation of antimicrobial activity was performed by microdilution method. RESULTS All compounds have shown antibacterial properties better than that of ampicillin and in many cases better than streptomycin. As far as the antifungal activity is concerned, all compounds possess much higher activity than reference drugs bifonazole and ketoconazole. The most sensitive bacterial species was B. cereus (MIC 6.5-28.4 µmol × 10-2/mL and MBC 14.2-105.0 µmol × 10-2/mL) while the most resistant ones were L. monocytogenes (MIC 21.4-113.6 µmol × 10-2/mL) and E. coli (MIC 10.7- 113.6 µmol × 10-2/mL) and MBC at 42.7-358.6 µmol × 10-2/mL and 21.4-247.2 µmol × 10-2/mL, respectively. All the compounds exhibited antibacterial activity against the three resistant strains, MRSA, P. aeruginosa and E.coli. with MIC and MBC in the range of 0.65-11.00 µmol/mL × 10-2 and 1.30-16.50 µmol/mL × 10-2. Docking studies were performed. CONCLUSION Twenty-eight novel thiazole-based chalcones were designed, synthesized and evaluated for antimicrobial activity. The results showed that these derivatives could be lead compounds in search of new potent antimicrobial agents. Docking studies indicated that DNA gyrase, GyrB and MurA inhibition may explain the antibacterial activity.",
journal = "Current Topics in Medicinal Chemistry",
title = "Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones.",
number = "5",
volume = "19",
doi = "10.2174/1568026619666190129121933",
pages = "356-375"
}

Tratrat, C., Haroun, M., Xenikakis, I., Liaras, K., Tsolaki, E., Eleftheriou, P., Petrou, A., Aldhubiab, B., Attimarad, M., Venugopala, K. N., Harsha, S., Elsewedy, H. S., Geronikaki, A.,& Soković, M.. (2019). Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones.. in Current Topics in Medicinal Chemistry, 19(5), 356-375.
https://doi.org/10.2174/1568026619666190129121933

Tratrat C, Haroun M, Xenikakis I, Liaras K, Tsolaki E, Eleftheriou P, Petrou A, Aldhubiab B, Attimarad M, Venugopala KN, Harsha S, Elsewedy HS, Geronikaki A, Soković M. Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones.. in Current Topics in Medicinal Chemistry. 2019;19(5):356-375.
doi:10.2174/1568026619666190129121933 .

Tratrat, Christophe, Haroun, Michelyne, Xenikakis, Iakovos, Liaras, Konstantinos, Tsolaki, Evangelia, Eleftheriou, Phaedra, Petrou, Anthi, Aldhubiab, Bandar, Attimarad, Mahesh, Venugopala, Katharigatta N., Harsha, Sree, Elsewedy, Heba S., Geronikaki, Athina, Soković, Marina, "Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones." in Current Topics in Medicinal Chemistry, 19, no. 5 (2019):356-375,
https://doi.org/10.2174/1568026619666190129121933 . .

TY  - JOUR
AU  - Tratrat, Christophe
AU  - Haroun, Michelyne
AU  - Paparisva, Aliki
AU  - Geronikaki, Athina
AU  - Camoutsis, Charalabos
AU  - Ćirić, Ana
AU  - Glamočlija, Jasmina
AU  - Soković, Marina
AU  - Fotakis, Charalmpos
AU  - Zoumpoulakis, Panagiotis
AU  - Bhunia, Shome
AU  - Saxena, Anil
PY  - 2018
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/4306
AB  - As a part of our ongoing studies in developing new derivatives as antimicrobial agents we
describe the synthesis of novel substituted 5-benzylideno-2-adamantylthiazol[3,2-b][1,2,4]triazol-6
(5H)ones.The twenty-five newly synthesized compounds were tested for their antimicrobial and
antifungal activity. All compounds have shown antibacterial properties with compounds 1–9 showing
the lowest activity, followed by compounds 10–14 while compounds 15–25 the highest antibacterial
activity. Specific compounds appeared to be more active than ampicillin in most studied
strains and in some cases more active than streptomycin. Antifungal activity in most cases also
was better than that of reference drugs ketoconazole and bifonazole. Elucidating the relation of molecular properties to antimicrobial activity as well as generation of pharmacophore model for
antifungal activity of two fungal species Aspergillus fumigatus and Candida albicans were performed.
PB  - Elsevier B.V. on behalf of King Saud University
T2  - Arabian Journal of Chemistry
T1  - Design, synthesis and biological evaluation of new substituted 5-benzylideno-2-adamantylthiazol[3,2- b][1,2,4]triazol-6(5H)ones. Pharmacophore models for antifungal activity
IS  - 4
VL  - 11
DO  - 10.1016/j.arabjc.2016.06.007
SP  - 573
EP  - 590
ER  - 

@article{
author = "Tratrat, Christophe and Haroun, Michelyne and Paparisva, Aliki and Geronikaki, Athina and Camoutsis, Charalabos and Ćirić, Ana and Glamočlija, Jasmina and Soković, Marina and Fotakis, Charalmpos and Zoumpoulakis, Panagiotis and Bhunia, Shome and Saxena, Anil",
year = "2018",
abstract = "As a part of our ongoing studies in developing new derivatives as antimicrobial agents we
describe the synthesis of novel substituted 5-benzylideno-2-adamantylthiazol[3,2-b][1,2,4]triazol-6
(5H)ones.The twenty-five newly synthesized compounds were tested for their antimicrobial and
antifungal activity. All compounds have shown antibacterial properties with compounds 1–9 showing
the lowest activity, followed by compounds 10–14 while compounds 15–25 the highest antibacterial
activity. Specific compounds appeared to be more active than ampicillin in most studied
strains and in some cases more active than streptomycin. Antifungal activity in most cases also
was better than that of reference drugs ketoconazole and bifonazole. Elucidating the relation of molecular properties to antimicrobial activity as well as generation of pharmacophore model for
antifungal activity of two fungal species Aspergillus fumigatus and Candida albicans were performed.",
publisher = "Elsevier B.V. on behalf of King Saud University",
journal = "Arabian Journal of Chemistry",
title = "Design, synthesis and biological evaluation of new substituted 5-benzylideno-2-adamantylthiazol[3,2- b][1,2,4]triazol-6(5H)ones. Pharmacophore models for antifungal activity",
number = "4",
volume = "11",
doi = "10.1016/j.arabjc.2016.06.007",
pages = "573-590"
}

Tratrat, C., Haroun, M., Paparisva, A., Geronikaki, A., Camoutsis, C., Ćirić, A., Glamočlija, J., Soković, M., Fotakis, C., Zoumpoulakis, P., Bhunia, S.,& Saxena, A.. (2018). Design, synthesis and biological evaluation of new substituted 5-benzylideno-2-adamantylthiazol[3,2- b][1,2,4]triazol-6(5H)ones. Pharmacophore models for antifungal activity. in Arabian Journal of Chemistry
Elsevier B.V. on behalf of King Saud University., 11(4), 573-590.
https://doi.org/10.1016/j.arabjc.2016.06.007

Tratrat C, Haroun M, Paparisva A, Geronikaki A, Camoutsis C, Ćirić A, Glamočlija J, Soković M, Fotakis C, Zoumpoulakis P, Bhunia S, Saxena A. Design, synthesis and biological evaluation of new substituted 5-benzylideno-2-adamantylthiazol[3,2- b][1,2,4]triazol-6(5H)ones. Pharmacophore models for antifungal activity. in Arabian Journal of Chemistry. 2018;11(4):573-590.
doi:10.1016/j.arabjc.2016.06.007 .

Tratrat, Christophe, Haroun, Michelyne, Paparisva, Aliki, Geronikaki, Athina, Camoutsis, Charalabos, Ćirić, Ana, Glamočlija, Jasmina, Soković, Marina, Fotakis, Charalmpos, Zoumpoulakis, Panagiotis, Bhunia, Shome, Saxena, Anil, "Design, synthesis and biological evaluation of new substituted 5-benzylideno-2-adamantylthiazol[3,2- b][1,2,4]triazol-6(5H)ones. Pharmacophore models for antifungal activity" in Arabian Journal of Chemistry, 11, no. 4 (2018):573-590,
https://doi.org/10.1016/j.arabjc.2016.06.007 . .

TY  - JOUR
AU  - Haroun, Michelyne
AU  - Tratrat, Christophe
AU  - Kositsi, Katerina
AU  - Tsolaki, Evangelia
AU  - Petrou, Anthi
AU  - Aldhubiab, Bandar
AU  - Attimarad, Mahesh
AU  - Harsha, Sree
AU  - Geronikaki, Athina
AU  - Venugopala, Katharigatta N.
AU  - Elsewedy, Heba S.
AU  - Soković, Marina
AU  - Glamočlija, Jasmina
AU  - Ćirić, Ana
PY  - 2018
UR  - http://www.eurekaselect.com/159582/article
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3071
AB  - BACKGROUND Thiazole and benzothiazole derivatives, as well as thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity. OBJECTIVE The goal of this paper is the designing of new benzothiazole based thiazolidinones and the evaluation of their biological activities. METHODS The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was evaluated using the method of microdilution. RESULTS The twelve newly synthesized compounds showed antimicrobial properties. All compounds appeared to be more active than ampicillin in most studied strains and in some cases, more active than streptomycin. Antifungal activity, in most cases was also better than the reference drugs ketoconazole and bifonazole. The prediction of cytotoxicity revealed that the synthesized compounds were not toxic (LD50 350-1000 mg/kg of body weight). Docking studies on the antibacterial activity confirmed the biological results. CONCLUSION The twelve new compounds were synthesized and studied for their antimicrobial activity. The compounds appeared to be promising antimicrobial agents and could be the lead compounds for new, more potent drugs. According to the docking prediction, the compounds could be MurB inhibitors.
T2  - Current Topics in Medicinal Chemistry
T1  - New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation.
IS  - 1
VL  - 18
DO  - 10.2174/1568026618666180206101814
SP  - 75
EP  - 87
ER  - 

@article{
author = "Haroun, Michelyne and Tratrat, Christophe and Kositsi, Katerina and Tsolaki, Evangelia and Petrou, Anthi and Aldhubiab, Bandar and Attimarad, Mahesh and Harsha, Sree and Geronikaki, Athina and Venugopala, Katharigatta N. and Elsewedy, Heba S. and Soković, Marina and Glamočlija, Jasmina and Ćirić, Ana",
year = "2018",
abstract = "BACKGROUND Thiazole and benzothiazole derivatives, as well as thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity. OBJECTIVE The goal of this paper is the designing of new benzothiazole based thiazolidinones and the evaluation of their biological activities. METHODS The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was evaluated using the method of microdilution. RESULTS The twelve newly synthesized compounds showed antimicrobial properties. All compounds appeared to be more active than ampicillin in most studied strains and in some cases, more active than streptomycin. Antifungal activity, in most cases was also better than the reference drugs ketoconazole and bifonazole. The prediction of cytotoxicity revealed that the synthesized compounds were not toxic (LD50 350-1000 mg/kg of body weight). Docking studies on the antibacterial activity confirmed the biological results. CONCLUSION The twelve new compounds were synthesized and studied for their antimicrobial activity. The compounds appeared to be promising antimicrobial agents and could be the lead compounds for new, more potent drugs. According to the docking prediction, the compounds could be MurB inhibitors.",
journal = "Current Topics in Medicinal Chemistry",
title = "New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation.",
number = "1",
volume = "18",
doi = "10.2174/1568026618666180206101814",
pages = "75-87"
}

Haroun, M., Tratrat, C., Kositsi, K., Tsolaki, E., Petrou, A., Aldhubiab, B., Attimarad, M., Harsha, S., Geronikaki, A., Venugopala, K. N., Elsewedy, H. S., Soković, M., Glamočlija, J.,& Ćirić, A.. (2018). New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation.. in Current Topics in Medicinal Chemistry, 18(1), 75-87.
https://doi.org/10.2174/1568026618666180206101814

Haroun M, Tratrat C, Kositsi K, Tsolaki E, Petrou A, Aldhubiab B, Attimarad M, Harsha S, Geronikaki A, Venugopala KN, Elsewedy HS, Soković M, Glamočlija J, Ćirić A. New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation.. in Current Topics in Medicinal Chemistry. 2018;18(1):75-87.
doi:10.2174/1568026618666180206101814 .

Haroun, Michelyne, Tratrat, Christophe, Kositsi, Katerina, Tsolaki, Evangelia, Petrou, Anthi, Aldhubiab, Bandar, Attimarad, Mahesh, Harsha, Sree, Geronikaki, Athina, Venugopala, Katharigatta N., Elsewedy, Heba S., Soković, Marina, Glamočlija, Jasmina, Ćirić, Ana, "New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation." in Current Topics in Medicinal Chemistry, 18, no. 1 (2018):75-87,
https://doi.org/10.2174/1568026618666180206101814 . .