Azaindoles: Noncovalent DprE1 Inhibitors from Scaffold Morphing Efforts, Kill Mycobacterium tuberculosis and Are Efficacious <i>in Vivo</i>

S. Shirude, Pravin; Krishan Shandil, Radha; Sadler, C; Naik, Maruti; Hosagrahara, Vinayak; Hameed, Shahul; Shinde, Vikas; Bathula, Chandramohan; Humnabadkar, Vaishali; Kumar, Naveen; Reddy, Jitendar; Panduga, Vijender; Sharma, Sreevalli; Ambady, Anisha; Hegde, Naina; Whiteaker, James; E. McLaughlin, Robert; Gardner, Humphrey; Madhavapeddi, Prashanti; Ramachandran, Vasanthi; Kaur, Parvinder; Narayan, Ashwini; Guptha, Supreeth; Awasthy, Disha; Narayan, Chandan; Mahadevaswamy, Jyothi; G. Vishwas, K.; Kamal Ahuja, Vijay; Srivastava, Abhishek; Prabhakar, KR; Bharath, Sowmya; R. Kale, Ramesh; Ramaiah, Manjunatha; Roy Choudhury, Nilanjana; K. Sambandamurthy, Vasan; Solapure, Suresh; S. Iyer, Pravin; Narayanan, Shridhar; Chatterji, Monalisa

doi:10.1021/jm401382v

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Azaindoles: Noncovalent DprE1 Inhibitors from Scaffold Morphing Efforts, Kill Mycobacterium tuberculosis and Are Efficacious in Vivo

Published in Journal of Medicinal Chemistry • Nov 11, 2013

Authors:

Pravin S. Shirude

Radha Krishan Shandil

C Sadler

Abstract

We report 1,4-azaindoles as a new inhibitor class that kills Mycobacterium tuberculosis in vitro and demonstrates efficacy in mouse tuberculosis models. The series emerged from scaffold morphing efforts and was demonstrated to noncovalently inhibit decaprenylphosphoryl-β-D-ribose2'-epimerase (DprE1)...

Subject

Mycobacterium tuberculosis

In vivo

Chemistry

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