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Targeting DNA Gyrase to Combat Mycobacterium tuberculosis: An Update

Author(s):

Swetarka Das, Tanu Garg, Nanduri Srinivas, Arunava Dasgupta and Sidharth Chopra*   Pages 1 - 15 ( 15 )

Abstract:


DNA gyrase is a clinically validated drug target, currently targeted only by fluoroquinolone class of antibacterials. However, owing to increasing drug resistance as well as concomitant reduction in availability of newer classes of antibiotics, fluoroquinolones are increasingly being over-utilized in order to treat serious infections, including multi-drug resistant tuberculosis. This in turn, increases the probability of resistance to fluoroquinolones, which is mediated by a single amino acid change in gyrA, leading to class wide resistance. In this review, we provide an overview on the recent progress in identifying novel scaffolds which target DNA gyrase and provide an update on their discovery and development status.

Keywords:

M. tuberculosis, DNA gyrase, Fluoroquinolones, aminocoumarins

Affiliation:

Division of Microbiology, CSIR-Central Drug Research Institute, Lucknow-226031, Uttar Pradesh, Division of Microbiology, CSIR-Central Drug Research Institute, Lucknow-226031, Uttar Pradesh, Department of Medicinal and Process Chemistry, National Institute of Pharmaceutical Education and Research, Hyderabad, Telangana, Division of Microbiology, CSIR-Central Drug Research Institute, Lucknow-226031, Uttar Pradesh, Division of Microbiology, CSIR-Central Drug Research Institute, Lucknow-226031, Uttar Pradesh



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