Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.

doi:10.1021/jm800856c

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Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.

Journal of medicinal chemistry - 23 Oct 2008

Tucker Thomas J, Sisko John T, Tynebor Robert M, Williams Theresa M, Felock Peter J, Flynn Jessica A, Lai Ming-Tain, Liang Yuexia, McGaughey Georgia, Liu Meiquing, Miller Mike, Moyer Gregory, Munshi Vandna, Perlow-Poehnelt Rebecca, Prasad Sridhar, Reid John C, Sanchez Rosa, Torrent Maricel, Vacca Joseph P, Wan Bang-Lin, Yan Youwei

Abstract excerpt

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have been shown to be a key component of highly active antiretroviral therapy (HAART). The use of NNRTIs has become part of standard combination antiviral therapies producing clinical outcomes with efficacy comparable to other antiviral regimens. There is, however, a critical issue with the emergence of clinical resistance, and a need has arisen for novel...

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PMID: 18826204
DOI: 10.1021/jm800856c

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