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

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)...

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Veröffentlicht in:	Journal of medicinal chemistry 2013-12, Vol.56 (23), p.9701-9708
Hauptverfasser:	Shirude, Pravin S, Shandil, Radha, Sadler, Claire, 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, McLaughlin, Robert E, Gardner, Humphrey, Madhavapeddi, Prashanti, Ramachandran, Vasanthi, Kaur, Parvinder, Narayan, Ashwini, Guptha, Supreeth, Awasthy, Disha, Narayan, Chandan, Mahadevaswamy, Jyothi, Vishwas, KG, Ahuja, Vijaykamal, Srivastava, Abhishek, Prabhakar, KR, Bharath, Sowmya, Kale, Ramesh, Ramaiah, Manjunatha, Choudhury, Nilanjana Roy, Sambandamurthy, Vasan K, Solapure, Suresh, Iyer, Pravin S, Narayanan, Shridhar, Chatterji, Monalisa
Format:	Artikel
Sprache:	eng
Schlagworte:	Alcohol Oxidoreductases Animals Antitubercular Agents - pharmacokinetics Antitubercular Agents - pharmacology Antitubercular Agents - therapeutic use Bacterial Proteins - antagonists & inhibitors Drug Discovery Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Enzyme Inhibitors - therapeutic use Indoles - chemical synthesis Indoles - pharmacokinetics Indoles - pharmacology Indoles - therapeutic use Mice Mycobacterium tuberculosis - drug effects Oxidoreductases - antagonists & inhibitors Rats Tuberculosis, Multidrug-Resistant - drug therapy
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