标题：The Synthesis and Antibacterial Activity of Novel 3-O-arylalkylbenzamide Derivatives as FtsZ Inhibitors
作者：Siti Ma;Rongmei Wang;Yuanze Wang;Jichao Cao Shutao Ma
作者机构：[Ma, S] Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, 44 West Cult 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：Antibacterial evaluation;3-O-Arylalkyl groups;Benzamide derivatives;FtsZ inhibitors;Resistant bacteria;Synthesis
摘要：A series of novel 3-O-arylalkylbenzamide derivatives as FtsZ inhibitors was designed, synthesized and evaluated for their cell division inhibitory activity against B. subtilis and S. aureus, and in vitro antibacterial activity against various phenotypes of Gram-positive bacteria. This series showed significantly improved on-target activity and in vitro antibacterial activity compared with 3-MBA. Among them, 3-O-alkylbenzamids 4–8 and 3-O-bromoalkylbenzamides 9 and 10 showed significantly improved activity against three phenotypes of S. aureus ATCC25923, S. aureusATCC29213 (MRSA) and S. aureus PR. Preliminary structure-activity relationships indicated that the extension of 3-O-alkyl side chain resulted in a substantial improvement in the antibacterial activity, and the small group like methyl or ethyl group at the position 1–3 of the 3-O-alkyl side chain did not affect the antibacterial activity while the large group such as benzene or heterocycle at the position 4 or 5 of the 3-O-alkyl side chain could lead to poor antibacterial activity.