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The study of 9,10-dihydroacridine derivatives as a new and effective molecular scaffold for antibacterial agent development
Biochemical and Biophysical Research Communications ( IF 2.5 ) Pub Date : 2021-02-06 , DOI: 10.1016/j.bbrc.2021.01.096
Cui-Cui Chen , Yi-Qi Zhang , Dong-Xiao Zhong , Xuan-He Huang , Yi-Han Zhang , Wen-Hao Jiang , Ming Li , Qian Chen , Wing-Leung Wong , Yu-Jing Lu

The emergence of worldwide spreading drug-resistant bacteria has been a serious threat to public health during the past decades. The development of new and effective antibacterial agents to address this critical issue is an urgent action. In the present study, we investigated the antibacterial activity of two 9,10-dihydroacridine derivatives and their mechanism. Both compounds were found possessing strong antibacterial activity against some selected Gram-positive bacteria including MRSA, VISA and VRE. The biological study suggests that the compounds promoted FtsZ polymerization and also disrupted Z-ring formation at the dividing site and consequently, the bacterial cell division is interrupted and causing cell death.



中文翻译:

9,10-二氢ac啶衍生物作为新型有效抗菌剂分子支架的研究

在过去的几十年中,耐药菌在全球范围内的传播一直严重威胁着公众健康。开发解决这一关键问题的新​​型有效抗菌剂是一项紧迫的任务。在本研究中,我们研究了两种9,10-二氢ac啶衍生物的抗菌活性及其机理。发现这两种化合物均对某些选定的革兰氏阳性细菌(包括MRSA,VISA和VRE)具有强大的抗菌活性。生物学研究表明,这些化合物促进了FtsZ聚合,并且还破坏了分裂位点的Z环形成,因此,细菌细胞分裂被中断并导致细胞死亡。

更新日期:2021-02-07
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