| Structural highlights
Publication Abstract from PubMed
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.
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.,Cote B, Burch JD, Asante-Appiah E, Bayly C, Bedard L, Blouin M, Campeau LC, Cauchon E, Chan M, Chefson A, Coulombe N, Cromlish W, Debnath S, Deschenes D, Dupont-Gaudet K, Falgueyret JP, Forget R, Gagne S, Gauvreau D, Girardin M, Guiral S, Langlois E, Li CS, Nguyen N, Papp R, Plamondon S, Roy A, Roy S, Seliniotakis R, St-Onge M, Ouellet S, Tawa P, Truchon JF, Vacca J, Wrona M, Yan Y, Ducharme Y Bioorg Med Chem Lett. 2014 Feb 1;24(3):917-22. doi: 10.1016/j.bmcl.2013.12.070., Epub 2013 Dec 24. PMID:24412110[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Cote B, Burch JD, Asante-Appiah E, Bayly C, Bedard L, Blouin M, Campeau LC, Cauchon E, Chan M, Chefson A, Coulombe N, Cromlish W, Debnath S, Deschenes D, Dupont-Gaudet K, Falgueyret JP, Forget R, Gagne S, Gauvreau D, Girardin M, Guiral S, Langlois E, Li CS, Nguyen N, Papp R, Plamondon S, Roy A, Roy S, Seliniotakis R, St-Onge M, Ouellet S, Tawa P, Truchon JF, Vacca J, Wrona M, Yan Y, Ducharme Y. Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses. Bioorg Med Chem Lett. 2014 Feb 1;24(3):917-22. doi: 10.1016/j.bmcl.2013.12.070., Epub 2013 Dec 24. PMID:24412110 doi:http://dx.doi.org/10.1016/j.bmcl.2013.12.070
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