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HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) are part of the combination therapy currently used to treat HIV infection. The features of a new NNRTI drug for HIV treatment must include selective potent activity against both wild-type virus as well as against mutant virus that have been selected by use of current antiretroviral treatment regimens. Based on analogy with known HIV-1 NNRTI inhibitors and modeling studies utilizing the X-ray crystal structure of inhibitors bound in the HIV-1 RT, a series of substituted 2-quinolones was synthesized and evaluated as HIV-1 inhibitors.

Original publication




Journal article


J Med Chem

Publication Date





5923 - 5936


Anti-HIV Agents, Benzoxazines, Binding Sites, Cell Line, Crystallography, X-Ray, Drug Design, Drug Resistance, Viral, HIV Reverse Transcriptase, HIV-1, Humans, Models, Molecular, Molecular Structure, Mutation, Oxazines, Quinolones, Reverse Transcriptase Inhibitors, Structure-Activity Relationship