Azaindoles: Noncovalent DprE1 Inhibitors from Scaffold Morphing Efforts, Kill Mycobacterium tuberculosis and Are Efficacious in Vivo
Journal of Medicinal Chemistry2013Vol. 56(23), pp. 9701–9708
Citations Over TimeTop 10% of 2013 papers
Pravin S. Shirude, Radha Krishan Shandil, C Sadler, Maruti Naik, Vinayak Hosagrahara, Shahul Hameed, Vikas Shinde, Chandramohan Bathula, Vaishali Humnabadkar, Naveen Kumar, Jitendar Reddy, Vijender Panduga, Sreevalli Sharma, Anisha Ambady, Naina Hegde, James Whiteaker, Robert E. McLaughlin, Humphrey Gardner, Prashanti Madhavapeddi, Vasanthi Ramachandran, Parvinder Kaur, Ashwini Narayan, Supreeth Guptha, Disha Awasthy, Chandan Narayan, Jyothi Mahadevaswamy, K. G. Vishwas, Vijay Kamal Ahuja, Abhishek Srivastava, KR Prabhakar, Sowmya Bharath, Ramesh R. Kale, Manjunatha Ramaiah, Nilanjana Roy Choudhury, Vasan K. Sambandamurthy, Suresh Solapure, Pravin S. Iyer, Shridhar Narayanan, Monalisa Chatterji
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). With "drug-like" properties and no expectation of pre-existing resistance in the clinic, this chemical class has the potential to be developed as a therapy for drug-sensitive and drug-resistant tuberculosis.
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