Article
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Journal of medicinal chemistry - 26 Jun 2014
Naik Maruti, Humnabadkar Vaishali, Tantry Subramanyam J, Panda Manoranjan, Narayan Ashwini, Guptha Supreeth, Panduga Vijender, Manjrekar Praveena, Jena Lalit Kumar, Koushik Krishna, Shanbhag Gajanan, Jatheendranath Sandesh, Manjunatha M R, Gorai Gopinath, Bathula Chandramohan, Rudrapatna Suresh, Achar Vijayashree, Sharma Sreevalli, Ambady Anisha, Hegde Naina, Mahadevaswamy Jyothi, Kaur Parvinder, Sambandamurthy Vasan K, Awasthy Disha, Narayan Chandan, Ravishankar Sudha, Madhavapeddi Prashanti, Reddy Jitendar, Prabhakar Kr, Saralaya Ramanatha, Chatterji Monalisa, Whiteaker James, McLaughlin Bob, Chiarelli Laurent R, Riccardi Giovanna, Pasca Maria Rosalia, Binda Claudia, Neres João, Dhar Neeraj, Signorino-Gelo François, McKinney John D, Ramachandran Vasanthi, Shandil Radha, Tommasi Ruben, Iyer Pravin S, Narayanan Shridhar, Hosagrahara Vinayak, Kavanagh Stefan, Dinesh Neela, Ghorpade Sandeep R
Abstract excerpt
4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequencing of mutants raised against AQs, identified decaprenylphosphoryl-β-d-ribose 2'-epimerase (DprE1) as the primary target responsible for the antitubercular...
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