Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies
2022
Authors:
Kartsev, VictorGeronikaki, Athina
Zubenko, Alexander
Petrou, Anthi
Ivanov, Marija
Glamočlija, Jasmina
Soković, Marina
Divaeva, Lyudmila
Morkovnik, Anatolii
Klimenko, Alexander
Document Type:
Article (Published version)
Metadata
Show full item recordAbstract:
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.
Keywords:
antibacterial; antifungal; antimicrobial; docking; heteroaryl (aryl) thiazole derivativesSource:
Antibiotics, 2022, 11, 10, 1337-Funding / projects:
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200007 (University of Belgrade, Institute for Biological Research 'Siniša Stanković') (RS-MESTD-inst-2020-200007)
- 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)
DOI: 10.3390/antibiotics11101337
ISSN: 2079-6382
PubMed: 36289995
WoS: 000872098000001
Scopus: 2-s2.0-85140478842
URI
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC9658463http://radar.ibiss.bg.ac.rs/handle/123456789/5173