Academic Journal
Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies
| العنوان: | Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies |
|---|---|
| المؤلفون: | Kartsev, Victor, Geronikaki, Athina, Zubenko, Alexander, Petrou, Anthi, Ivanov, Marija, Glamočlija, Jasmina, Soković, Marina, Divaeva, Lyudmila, Morkovnik, Anatolii, Klimenko, Alexander |
| المصدر: | Antibiotics |
| بيانات النشر: | MDPI |
| سنة النشر: | 2022 |
| المجموعة: | RADaR - Digital Repository of Archived Publications Institute for Biological Research "Sinisa Stankovic" / РАДаР - Репозиторијум Архивираних Дигиталних Радова Институт за биолошка истраживања "Синиша Станковић" |
| مصطلحات موضوعية: | antibacterial, antifungal, antimicrobial, docking, heteroaryl (aryl) thiazole derivatives |
| الوصف: | 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. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | unknown |
| تدمد: | 2079-6382 |
| Relation: | info:eu-repo/grantAgreement/MESTD/inst-2020/200007/RS//; Fundamental Scientific Research of the State Academies of Sciences for 2014-2021 (grant no. 0710-2019-0044); Ministry of Science and Higher Education of the Russian Federation (Southern Federal University, 2020, project FENW-2020-0031); http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC9658463; http://radar.ibiss.bg.ac.rs/handle/123456789/5173; 2-s2.0-85140478842; 000872098000001; https://radar.ibiss.bg.ac.rs/bitstream/id/11309/antibiotics-11-01337.pdf |
| DOI: | 10.3390/antibiotics11101337 |
| الاتاحة: | http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC9658463 http://radar.ibiss.bg.ac.rs/handle/123456789/5173 https://doi.org/10.3390/antibiotics11101337 https://radar.ibiss.bg.ac.rs/bitstream/id/11309/antibiotics-11-01337.pdf |
| Rights: | openAccess ; https://creativecommons.org/licenses/by/4.0/ ; BY ; © 2022 by the authors. Licensee MDPI, Basel, Switzerland. |
| رقم الانضمام: | edsbas.9E507439 |
| قاعدة البيانات: | BASE |
Full Text Finder | تدمد: | 20796382 |
|---|---|
| DOI: | 10.3390/antibiotics11101337 |