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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Côté B,Burch JD,Asante-Appiah E,Bayly C,Bédard L,Blouin M,Campeau LC,Cauchon E,Chan M,Chefson A,Coulombe N,Cromlish W,Debnath S,Deschênes D,Dupont-Gaudet K,Falgueyret JP,Forget R,Gagné S,Gauvreau D,Girardin M,Guir

doi

10.1016/j.bmcl.2013.12.070

subject

Has Abstract

pub_date

2014-02-01 00:00:00

pages

917-22

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)01454-6

journal_volume

24

pub_type

杂志文章

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