Synthesis and Antibiotic Activity Study of Pyridine Chalcone Derivatives against Methicillin-Resistant Staphylococcus aureus

Abstract

A series of pyridine chalcone derivatives were designed and synthesized. The structures were confirmed by 1 H NMR, 13 C NMR and HRMS. In vitro biological activity evaluation results showed that five of the compounds exhibited good biological activity against gram positive bacteria staphylococcus aureus (ATCC 29213). Further antibiotic activity of these five compounds against 11 clinical isolated methicillin-resistant staphylococcus aureus (MRSA) were evaluated. The results showed that four of the compounds exhibited good antibacterial activity against MRSA. (E)-2-Bromo-N-{4-[3-(pyridin-2-yl)acryloyl]phenyl}acetamide (5k) showed the most effective activity (minimum inhibitory concentration, MIC＝4 μg/mL). In terms of hemolytic activity evaluation, compound 5k showed virtually no toxicity even in 1000 μg/mL concentration. To sum up, pyridine chalcone 5k was potential for further antibiotic study as anti-MRSA agent.

Synthesis and Antibacterial Activity Evaluation of Imidazole Derivatives Containing 6‐Methylpyridine Moiety

“…These compounds showed good activity against Gram‐positive and Gram‐negative bacteria, and compound 2 showed very high activity against both Gram‐positive and Gram‐negative bacteria with a MIC value of 0.24 μg/mL. In addition, we found that compounds with imidazole ( 3 [35] and 4 [36] ) and pyridine ( 5 [37] and 6 [38] ) structures showed good antibacterial and antifungal activities.…”