Novel Bacterial Topoisomerase inhibitors (NBTIs) - A comprehensive review
European Journal of Medicinal Chemistry Reports(2021)
Abstract
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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Key words
DNA gyrase,hERG,MIC,NBTI,Topoisomerase
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