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Azaindoles: noncovalent DprE1 inhibitors from scaffold morphing efforts, kill Mycobacterium tuberculosis and are efficacious in vivo.
Shirude PS, Shandil R, Sadler C, Naik M, Hosagrahara V, Hameed S, Shinde V, Bathula C, Humnabadkar V, Kumar N, Reddy J, Panduga V, Sharma S, Ambady A, Hegde N, Whiteaker J, McLaughlin RE, Gardner H, Madhavapeddi P, Ramachandran V, Kaur P, Narayan A, Guptha S, Awasthy D, Narayan C, Mahadevaswamy J, Vishwas KG, Ahuja V, Srivastava A, Prabhakar KR, Bharath S, Kale R, Ramaiah M, Choudhury NR, Sambandamurthy VK, Solapure S, Iyer PS, Narayanan S, Chatterji M. Shirude PS, et al. J Med Chem. 2013 Dec 12;56(23):9701-8. doi: 10.1021/jm401382v. Epub 2013 Nov 21. J Med Chem. 2013. PMID: 24215368
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
Shirude PS, Shandil RK, Manjunatha MR, Sadler C, Panda M, Panduga V, Reddy J, Saralaya R, Nanduri R, Ambady A, Ravishankar S, Sambandamurthy VK, Humnabadkar V, Jena LK, Suresh RS, Srivastava A, Prabhakar KR, Whiteaker J, McLaughlin RE, Sharma S, Cooper CB, Mdluli K, Butler S, Iyer PS, Narayanan S, Chatterji M. Shirude PS, et al. J Med Chem. 2014 Jul 10;57(13):5728-37. doi: 10.1021/jm500571f. Epub 2014 Jun 20. J Med Chem. 2014. PMID: 24874895
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
Hameed P S, Patil V, Solapure S, Sharma U, Madhavapeddi P, Raichurkar A, Chinnapattu M, Manjrekar P, Shanbhag G, Puttur J, Shinde V, Menasinakai S, Rudrapatana S, Achar V, Awasthy D, Nandishaiah R, Humnabadkar V, Ghosh A, Narayan C, Ramya VK, Kaur P, Sharma S, Werngren J, Hoffner S, Panduga V, Kumar CN, Reddy J, Kumar K N M, Ganguly S, Bharath S, Bheemarao U, Mukherjee K, Arora U, Gaonkar S, Coulson M, Waterson D, Sambandamurthy VK, de Sousa SM. Hameed P S, et al. J Med Chem. 2014 Jun 12;57(11):4889-905. doi: 10.1021/jm500432n. Epub 2014 May 23. J Med Chem. 2014. PMID: 24809953
107 results