Litcius/Paper detail

Novel Bacterial Topoisomerase inhibitors (NBTIs) – A comprehensive review

Jigar Desai, S Sachchidanand, Sanjay Kumar, Rajiv Sharma

2021European Journal of Medicinal Chemistry Reports27 citationsDOIOpen Access PDF

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.

Topics & Concepts

DNA gyraseTopoisomeraseTopoisomerase IVBacteriaAntibioticsTopoisomerase inhibitorMechanism of actionChemistryAntibiotic resistanceMicrobiologyDNABiologyComputational biologyBiochemistryEscherichia coliGeneticsIn vitroGeneCancer therapeutics and mechanismsAntibiotic Resistance in BacteriaAntibiotics Pharmacokinetics and Efficacy