Synthesis of some new 2-(3-pyridyl)-4,5-disubstituted thiazoles as potent antimicrobial agents.

Eur J Med Chem

Department of Chemistry, Faculty of Science, Mansoura University, ET-35516 Mansoura, Egypt.

Published: April 2013

As a part of ongoing studies in developing new potent antimicrobial agents, a series of novel 2-(3-pyridyl)-4,5-disubstituted thiazoles was efficiently synthesized and characterized by spectral and elemental analyses. The newly synthesized compounds were evaluated for their in vitro antimicrobial activity against ten bacterial and five fungal human pathogenic strains using the disc diffusion assay. Among the synthesized compounds, 5-acetyl-4-methyl-2-(3-pyridyl)thiazole (5) exhibited twofold antibacterial activity of ampicillin in inhibiting the growth of Staphylococcus epidermidis (MIC 0.24 μg/mL) and also showed equipotent antifungal activity with amphotricin B against Geotricum candidum (MIC 0.48 μg/mL). From structure-activity relationship (SAR) point of view, increasing the size of the substitutions either at position 4 or 5 on the thiazole nucleus decreased the antimicrobial activity.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejmech.2012.12.050DOI Listing

Publication Analysis

Top Keywords

2-3-pyridyl-45-disubstituted thiazoles
8
potent antimicrobial
8
antimicrobial agents
8
synthesized compounds
8
antimicrobial activity
8
synthesis 2-3-pyridyl-45-disubstituted
4
thiazoles potent
4
antimicrobial
4
agents ongoing
4
ongoing studies
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!