Phenylimidazole derivatives as new inhibitors of bacterial enoyl-ACP reductase FabK

Novel FabK inhibitors with antibacterial activity against Streptococcus pneumoniae were synthesized and evaluated. Through SAR studies of our initial hit compound 2-(1H-benz[d]imidazol-2-ylthio)-N-(6-methoxycarbonylbenzo[d]thiazol-2-yl)acetamide, a series of novel phenylimidazole derivatives were discovered as potent FabK inhibitors.

Graphical abstractWe discovered the phenylimidazole derivative as a novel inhibitor of bacterial enoyl-ACP reductase (FabK). It selectively exhibited strong FabK-inhibitory activity and good antibacterial activities against Streptococcus pneumoniae.Figure optionsDownload full-size imageDownload as PowerPoint slide