Synthesis and on-target antibacterial activity of novel 3-elongated arylalkoxybenzamide derivatives as inhibitors of the bacterial cell division protein FtsZ |
| |
| Authors: | Siti Ma Chao Cong Xiaohui Meng Shasha Cao Hongkun Yang Yuanyuan Guo Xueyi Lu Shutao Ma |
| |
| Affiliation: | 1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012, PR China;2. Institute of Diagnostics, School of Medicine, Shandong University, 44, West Culture Road, Jinan 250012, PR China |
| |
| Abstract: | Novel 3-elongated arylalkoxybenzamide derivatives were designed, synthesized and evaluated for their cell division inhibitory activity and antibacterial activity. Among them, the subseries of 3-alkyloxybenzamide derivatives exhibited greatly improved on-target activity against Bacillus subtilis and Staphylococcus aureus, and remarkably increased antibacterial activity against B. subtilis ATCC9372, penicillin-susceptible S. aureus ATCC25923, methicillin-resistant S. aureus ATCC29213 (MRSA) and penicillin-resistant S. aureus PR compared with 3-methoxybenzamide. In contrast, the subseries of 3-phenoxyaklyloxybenzamide, 3-heteroarylalkyloxybenzamide and 3-heteroarylthioalkyloxybenzamide derivatives only showed a significant improvement in on-target activity and antibacterial activity against B. subtilis ATCC9372. |
| |
| Keywords: | Arylalkoxybenzamide FtsZ inhibitors Synthesis Cell division inhibition activity Antibacterial activity |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
