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

doi:10.1016/j.bmcl.2013.12.070

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Article

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

Bioorganic & medicinal chemistry letters - 1 Feb 2014

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

Abstract excerpt

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....

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PMID: 24412110
DOI: 10.1016/j.bmcl.2013.12.070

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

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