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 . .