Novel Benzophenones as Non-nucleoside Reverse Transcriptase Inhibitors of HIV-1

Abstract

GW4511, GW4751, and GW3011 showed IC₅₀ values ≤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.