Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.

J W Corbett, K J Kresge, S Pan, B C Cordova, R M Klabe, J D Rodgers, S K Erickson-Viitanen

Journal: Bioorganic & medicinal chemistry letters 2001;11(3):309-12

PMID: 11212098

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Abstract

3-Alkoxymethyl- and 3-aryloxymethyl-2-pyridinones were synthesized and evaluated for activity as non-nucleoside reverse transcriptase inhibitors (NNRTIs) of HIV-1. It was found that several compounds were potent inhibitors of HIV-1 with the most potent compound 24 exhibiting an IC90 = 32 nM. Compound 24 also possessed a potent resistance profile as demonstrated by submicromolar IC90s against several clinically meaningful mutant virus strains.

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DOI: 10.1016/s0960-894x(00)00662-4