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Updated: Mar 1, 2026

System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
Published on: April 5, 2017
Identification and synthesis of novel inhibitors of mycobacterium ATP synthase
Yogesh B Surase1, Kirandeep Samby1, Sagar R Amale1
1New Drug Discovery Research, Ranbaxy Research Laboratories (Now Sun Pharmaceutical Industries Ltd.), Plot-20, Sector-18, Udyog Vihar, Gurgaon 122001, India; Daiichi Sankyo Life Science Research Centre in India, Daiichi Sankyo India Pharma Pvt. Ltd., Village Sarhaul, Sector-18, Udyog Vihar Industrial Area, Gurgaon 122 015, India.
Abstract:
A non-diaryl quinoline scaffold 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one was identified by screening of diverse set of compounds against M. smegmatis ATP synthase. Herein, we disclose our efforts to develop the structure activity relationship against Mycobacterium tuberculosis (Mtb.H37Rv strain) around the identified hit 1. A scaffold hopping approach was used to identify compounds 14a, 14b and 24a with improved activity against MTb.H37Rv.
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