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.
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收藏
页数：16
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