Article
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
Journal of medicinal chemistry - 12 Jun 2014
Panda Manoranjan, Ramachandran Sreekanth, Ramachandran Vasanthi, Shirude Pravin S, Humnabadkar Vaishali, Nagalapur Kavitha, Sharma Sreevalli, Kaur Parvinder, Guptha Supreeth, Narayan Ashwini, Mahadevaswamy Jyothi, Ambady Anisha, Hegde Naina, Rudrapatna Suresh S, Hosagrahara Vinayak P, Sambandamurthy Vasan K, Raichurkar Anandkumar
Abstract excerpt
A novel pyrazolopyridone class of inhibitors was identified from whole cell screening against Mycobacterium tuberculosis (Mtb). The series exhibits excellent bactericidality in vitro, resulting in a 4 log reduction in colony forming units following compound exposure. The significant modulation of minimum inhibitory concentration (MIC) against a Mtb strain overexpressing the Rv3790 gene suggested the target of...
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