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
DOI:10.2174/1570180811310040005
日期:2013.3.1
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
设计,合成和评估了一系列新颖的3-O-芳基烷基苯甲酰胺衍生物作为FtsZ抑制剂,它们对枯草芽孢杆菌和金黄色葡萄球菌具有细胞分裂抑制活性,并且对革兰氏阳性细菌的各种表型具有体外抗菌活性。与3-MBA相比,该系列药物的靶向活性和体外抗菌活性显着提高。其中,3-O-烷基苯甲酰胺4-8和3-O-溴烷基苯甲酰胺9和10对金黄色葡萄球菌ATCC25923,金黄色葡萄球菌ATCC29213(MRSA)和金黄色葡萄球菌PR的三种表型显示出显着改善的活性。初步的结构活性关系表明,3-O-烷基侧链的延长导致抗菌活性大大提高,