Novel Bacterial Topoisomerase inhibitors (NBTIs) - A comprehensive review

被引:17
|
作者
Desai, Jigar [1 ]
Sachchidanand, S. [1 ]
Kumar, Sanjay [1 ]
Sharma, Rajiv [1 ]
机构
[1] Zydus Res Ctr, Sarkhej Bavla NH 8A, Ahmadabad 382213, Gujarat, India
关键词
DNA gyrase; hERG; MIC; NBTI; Topoisomerase; SPECTRUM ANTIBACTERIAL AGENTS; DNA GYRASE; POTENT INHIBITORS; ESCHERICHIA-COLI; PHYSICOCHEMICAL PROPERTIES; II TOPOISOMERASES; TRICYCLICS E.G; HERG; SAR; DERIVATIVES;
D O I
10.1016/j.ejmcr.2021.100017
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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.
引用
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页数:16
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