DNA旋转酶
拓扑异构酶
拓扑异构酶
细菌
抗生素
拓扑异构酶抑制剂
作用机理
化学
抗生素耐药性
微生物学
DNA
生物
计算生物学
生物化学
大肠杆菌
遗传学
体外
基因
作者
Jigar Desai,S. Sachchidanand,Sanjay Kumar,Rajiv Sharma
标识
DOI:10.1016/j.ejmcr.2021.100017
摘要
Bacterial DNA gyrase and topoisomerase IV inhibition has emerged as a promising strategy for the cure of infections caused by antibiotic-resistant bacteria. Small molecule antibacterials inhibiting bacterial topoisomerases have been previously exploited by the successful fluoroquinolone class. The Novel Bacterial Topoisomerase Inhibitors (NBTIs) bind to a different site to that of the fluoroquinolones with novel mechanism of action to evade the existing target-mediated bacterial resistance associated with fluoroquinolones. This review comprehensively summarizes various efforts with respect to structural modifications of inhibitors and their impact on their general physicochemical and biological properties.
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