Abstract
Diaryl ether family as one of the promising second generation HIV-1 non-nucleoside reverse transcriptase inhibitors has attracted considerable attention over the past few years, among which clinical candidate MK-4965 has been advanced into phase II clinical trials. The successful development of diaryl ether family provides valuable avenues in traditional medicinal chemistry, crystallography and computer-aided drug design fields for the design of other novel anti-HIV drug candidates. In this review, the development of diaryl ether family is present including the evolutionary history, design strategies, extensive structural modifications, structure-activity relationship studies and computer-aided molecular simulation of the binding mode in detail.
Keywords: HIV-1, NNRTIs, diaryl ether, MK-4965, molecular simulation, drug design