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- Title
Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies.
- Authors
Kartsev, Victor; Geronikaki, Athina; Zubenko, Alexander; Petrou, Anthi; Ivanov, Marija; Glamočlija, Jasmina; Sokovic, Marina; Divaeva, Lyudmila; Morkovnik, Anatolii; Klimenko, Alexander
- Abstract
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.
- Subjects
THIAZOLE derivatives; MOLECULAR docking; ANTI-infective agents; METHICILLIN-resistant staphylococcus aureus; ESCHERICHIA coli
- Publication
Antibiotics (2079-6382), 2022, Vol 11, Issue 10, pN.PAG
- ISSN
2079-6382
- Publication type
Article
- DOI
10.3390/antibiotics11101337