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. 2014 Feb 1;24(3):917-22.
doi: 10.1016/j.bmcl.2013.12.070. Epub 2013 Dec 24.

Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses

Bernard Côté  1 , Jason D Burch  2 , Ernest Asante-Appiah  2 , Chris Bayly  2 , Leanne Bédard  2 , Marc Blouin  2 , Louis-Charles Campeau  2 , Elizabeth Cauchon  2 , Manuel Chan  2 , Amandine Chefson  2 , Nathalie Coulombe  2 , Wanda Cromlish  2 , Smita Debnath  2 , Denis Deschênes  2 , Kristina Dupont-Gaudet  2 , Jean-Pierre Falgueyret  2 , Robert Forget  2 , Sébastien Gagné  2 , Danny Gauvreau  2 , Melina Girardin  2 , Sébastien Guiral  2 , Eric Langlois  2 , Chun Sing Li  2 , Natalie Nguyen  2 , Rob Papp  2 , Serge Plamondon  2 , Amélie Roy  2 , Stéphanie Roy  2 , Ria Seliniotakis  2 , Miguel St-Onge  2 , Stéphane Ouellet  2 , Paul Tawa  2 , Jean-François Truchon  2 , Joe Vacca  2 , Marc Wrona  2 , Youwei Yan  3 , Yves Ducharme  2
Affiliations

Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses

Bernard Côté et al. Bioorg Med Chem Lett. .

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.

Keywords: HIV; Inhibitor; Non-nucleoside reverse transcriptase; Pyridone; Triazolinone.

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