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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY REPORTS | 2021年 / 3卷

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

页数：16

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