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J Med Chem. 2004 Feb 26;47(5):1175-82.

Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.

Author information

1
GlaxoSmithKline Inc., 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. joe.h.chan@gsk.com

Abstract

GW4511, GW4751, and GW3011 showed IC50 values < or =2 nM against wild type HIV-1 and <10 nM against 16 mutants. They were particularly potent against NNRTI-resistant viruses containing Y181C-, K103N-, and K103N-based double mutations, which account for a significant proportion of the clinical failure of the three currently marketed NNRTIs. The antiviral data together with the favorable pharmacokinetic data of GW4511 suggested that these benzophenones possess attributes of a new NNRTI drug candidate.

PMID:
14971897
DOI:
10.1021/jm030255y
[Indexed for MEDLINE]

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