TY  - JOUR
AU  - Fesatidou, Maria
AU  - Zagaliotis, Panagiotis
AU  - Camoutsis, Charalampos
AU  - Petrou, Anthi
AU  - Eleftheriou, Phaedra
AU  - Tratrat, Christophe
AU  - Haroun, Micheline
AU  - Geronikaki, Athina
AU  - Ćirić, Ana
AU  - Soković, Marina
PY  - 2018
UR  - https://www.sciencedirect.com/science/article/pii/S0968089618310277?via%3Dihub
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3127
AB  - In continuation of our efforts to develop new compounds with antimicrobial properties we describe design, synthesis, molecular docking study and evaluation of antimicrobial activity of seventeen novel 2-{[5-(adamantan-1-yl)-1,3,4-thiadiazol-2-yl]-imino}-5-arylidene-1,3-thiazolidin-4-ones. All compounds showed antibacterial activity against eight Gram positive and Gram negative bacterial species. Twelve out of seventeen compounds were more potent than streptomycin and all compounds exhibited higher potency than ampicillin. Compounds were also tested against three resistant bacterial strains: MRSA, P. aeruginosa and E. coli. The best antibacterial potential against ATCC and resistant strains was observed for compound 8 (2-{[5-(adamantan-1-yl)-1,3,4-thiadiazol-2-yl]-imino}-5-(4-nitrobenzylidene)-1,3thiazolidin-4-one). The most sensitive bacterium appeared to be S. typhimirium, followed by B. cereus while L. monocitogenes and M. flavus were the most resistant. Compounds were also tested for their antifungal activity against eight fungal species. All compounds exhibited antifungal activity better than the reference drugs bifonazole and ketokonazole (3-115 times). It was found that compound 8 appeared again to be the most potent. Molecular docking studies on E. coli MurB, MurA as well as C. albicans CYP 51 and dihydrofolate reductase were used for the prediction of mechanism of antibacterial and antifungal activities confirming the experimental results.
T2  - Bioorganic & Medicinal Chemistry
T1  - 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation.
DO  - 10.1016/j.bmc.2018.08.004
ER  - 

@article{
author = "Fesatidou, Maria and Zagaliotis, Panagiotis and Camoutsis, Charalampos and Petrou, Anthi and Eleftheriou, Phaedra and Tratrat, Christophe and Haroun, Micheline and Geronikaki, Athina and Ćirić, Ana and Soković, Marina",
year = "2018",
abstract = "In continuation of our efforts to develop new compounds with antimicrobial properties we describe design, synthesis, molecular docking study and evaluation of antimicrobial activity of seventeen novel 2-{[5-(adamantan-1-yl)-1,3,4-thiadiazol-2-yl]-imino}-5-arylidene-1,3-thiazolidin-4-ones. All compounds showed antibacterial activity against eight Gram positive and Gram negative bacterial species. Twelve out of seventeen compounds were more potent than streptomycin and all compounds exhibited higher potency than ampicillin. Compounds were also tested against three resistant bacterial strains: MRSA, P. aeruginosa and E. coli. The best antibacterial potential against ATCC and resistant strains was observed for compound 8 (2-{[5-(adamantan-1-yl)-1,3,4-thiadiazol-2-yl]-imino}-5-(4-nitrobenzylidene)-1,3thiazolidin-4-one). The most sensitive bacterium appeared to be S. typhimirium, followed by B. cereus while L. monocitogenes and M. flavus were the most resistant. Compounds were also tested for their antifungal activity against eight fungal species. All compounds exhibited antifungal activity better than the reference drugs bifonazole and ketokonazole (3-115 times). It was found that compound 8 appeared again to be the most potent. Molecular docking studies on E. coli MurB, MurA as well as C. albicans CYP 51 and dihydrofolate reductase were used for the prediction of mechanism of antibacterial and antifungal activities confirming the experimental results.",
journal = "Bioorganic & Medicinal Chemistry",
title = "5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation.",
doi = "10.1016/j.bmc.2018.08.004"
}

Fesatidou, M., Zagaliotis, P., Camoutsis, C., Petrou, A., Eleftheriou, P., Tratrat, C., Haroun, M., Geronikaki, A., Ćirić, A.,& Soković, M.. (2018). 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation.. in Bioorganic & Medicinal Chemistry.
https://doi.org/10.1016/j.bmc.2018.08.004

Fesatidou M, Zagaliotis P, Camoutsis C, Petrou A, Eleftheriou P, Tratrat C, Haroun M, Geronikaki A, Ćirić A, Soković M. 5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation.. in Bioorganic & Medicinal Chemistry. 2018;.
doi:10.1016/j.bmc.2018.08.004 .

Fesatidou, Maria, Zagaliotis, Panagiotis, Camoutsis, Charalampos, Petrou, Anthi, Eleftheriou, Phaedra, Tratrat, Christophe, Haroun, Micheline, Geronikaki, Athina, Ćirić, Ana, Soković, Marina, "5-Adamantan thiadiazole-based thiazolidinones as antimicrobial agents. Design, synthesis, molecular docking and evaluation." in Bioorganic & Medicinal Chemistry (2018),
https://doi.org/10.1016/j.bmc.2018.08.004 . .