| Literature DB >> 24412110 |
Bernard Côté1, Jason D Burch2, Ernest Asante-Appiah2, Chris Bayly2, Leanne Bédard2, Marc Blouin2, Louis-Charles Campeau2, Elizabeth Cauchon2, Manuel Chan2, Amandine Chefson2, Nathalie Coulombe2, Wanda Cromlish2, Smita Debnath2, Denis Deschênes2, Kristina Dupont-Gaudet2, Jean-Pierre Falgueyret2, Robert Forget2, Sébastien Gagné2, Danny Gauvreau2, Melina Girardin2, Sébastien Guiral2, Eric Langlois2, Chun Sing Li2, Natalie Nguyen2, Rob Papp2, Serge Plamondon2, Amélie Roy2, Stéphanie Roy2, Ria Seliniotakis2, Miguel St-Onge2, Stéphane Ouellet2, Paul Tawa2, Jean-François Truchon2, Joe Vacca2, Marc Wrona2, Youwei Yan3, Yves Ducharme2.
Abstract
The optimization of a novel series of non-nucleoside reverse transcriptase inhibitors (NNRTI) led to the identification of pyridone 36. In cell cultures, this new NNRTI shows a superior potency profile against a range of wild type and clinically relevant, resistant mutant HIV viruses. The overall favorable preclinical pharmacokinetic profile of 36 led to the prediction of a once daily low dose regimen in human. NNRTI 36, now known as MK-1439, is currently in clinical development for the treatment of HIV infection.Entities:
Keywords: HIV; Inhibitor; Non-nucleoside reverse transcriptase; Pyridone; Triazolinone
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Year: 2013 PMID： 24412110 DOI： 10.1016/j.bmcl.2013.12.070
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823