Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594869 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
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.
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Authors
Bernard Côté, Jason D. Burch, Ernest Asante-Appiah, Chris Bayly, Leanne Bédard, Marc Blouin, Louis-Charles Campeau, Elizabeth Cauchon, Manuel Chan, Amandine Chefson, Nathalie Coulombe, Wanda Cromlish, Smita Debnath, Denis Deschênes,