Article
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
Journal of medicinal chemistry - 26 Feb 2004
Chan Joseph H, Freeman George A, Tidwell Jeffrey H, Romines Karen R, Schaller Lee T, Cowan Jill R, Gonzales Steve S, Lowell Gina S, Andrews C W, Reynolds David J, St Clair Marty, Hazen Richard J, Ferris Rob G, Creech Katrina L, Roberts Grace B, Short Steven A, Weaver Kurt, Koszalka George W, Boone Lawrence R
Abstract excerpt
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...
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