| Literature DB >> 24215368 |
Pravin S Shirude1, Radha Shandil, Claire 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, Vijaykamal Ahuja, Abhishek Srivastava, K R Prabhakar, Sowmya Bharath, Ramesh 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.Entities:
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Year: 2013 PMID： 24215368 DOI： 10.1021/jm401382v
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446