标题：Phenylacrylamides as Novel FtsZ-targeted Potential Antimicrobials
作者：Li, Xin;Sheng, Juzheng;Song, Di;Guo, Liwei;Ma, Shutao
作者机构：[Li, X] Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan, 250012, China;[ Sheng, 更多
通讯作者地址：[Ma, ST]Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, 44 West Culture Rd, Jinan 250012, Peoples R China.
来源：Letters in drug design & discovery
关键词：2-methylbenzimidazolyl group;antibacterial activity;cell division inhibitory activity;FtsZ;phenylacrylamides;synthesis
摘要：A novel series of FtsZ-targeted phenylacrylamides were designed, synthesized and evaluated for their antibacterial activity and cell division inhibitory activity against various Gram-positive and -negative strains. Among them, some compounds displayed preferable or comparable antibacterial activity and cell division inhibitory activity in comparison with their parent cinnamic acid. In particular, the compounds bearing 2-methylbenzimidazolyl groups showed more potent antibacterial activity than the others against the tested strains. For instance, compound 12 exhibited over 32-fold more potent antibacterial activity than cinnamic acid against Staphylococcus epidermidis and compound 16 exerted over 32-fold better antibacterial activity against Staphylococcus aureus ATCC25923 and S. epidermidis than cinnamic acid. In contrast, against Bacillus subtilis ATCC9372, Escherichia coli ATCC25922 and Pseudomonas aeruginosa ATCC27853, the phenylacrylamides showed little or no antibacterial activity. In the cell division inhibitory activity, compounds 14-17 displayed more significant on-target activity against S. aureus ATCC25923 than the other tested strains. In particular, the most active compound 14 shared the minimum cell division concentration of 0.5 mu g/mL, which had over 256-fold better activity than all the references.