Novel Bacterial Topoisomerase inhibitors (NBTIs) – A comprehensive review

Autor: Jigar Desai, Sanjay Kumar, Rajiv Sharma, S. Sachchidanand
Rok vydání: 2021
Předmět:
Zdroj: European Journal of Medicinal Chemistry Reports, Vol 3, Iss, Pp 100017-(2021)
ISSN: 2772-4174
DOI: 10.1016/j.ejmcr.2021.100017
Popis: 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.
Databáze: OpenAIRE