Article
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
Journal of medicinal chemistry - 12 Jun 2014
Hameed P Shahul, Patil Vikas, Solapure Suresh, Sharma Umender, Madhavapeddi Prashanti, Raichurkar Anandkumar, Chinnapattu Murugan, Manjrekar Praveena, Shanbhag Gajanan, Puttur Jayashree, Shinde Vikas, Menasinakai Sreenivasaiah, Rudrapatana Suresh, Achar Vijayashree, Awasthy Disha, Nandishaiah Radha, Humnabadkar Vaishali, Ghosh Anirban, Narayan Chandan, Ramya V K, Kaur Parvinder, Sharma Sreevalli, Werngren Jim, Hoffner Sven, Panduga Vijender, Kumar C N Naveen, Reddy Jitendar, Kumar K N Mahesh, Ganguly Samit, Bharath Sowmya, Bheemarao Ugarkar, Mukherjee Kakoli, Arora Uma, Gaonkar Sheshagiri, Coulson Michelle, Waterson David, Sambandamurthy Vasan K, de Sousa Sunita M
Abstract excerpt
DNA gyrase is a clinically validated target for developing drugs against Mycobacterium tuberculosis (Mtb). Despite the promise of fluoroquinolones (FQs) as anti-tuberculosis drugs, the prevalence of pre-existing resistance to FQs is likely to restrict their clinical value. We describe a novel class of N-linked aminopiperidinyl alkyl quinolones and naphthyridones that kills Mtb by inhibiting the DNA gyrase...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.