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

…, RM Klabe, JD Rodgers, SK Erickson-Viitanen

Index: Corbett, Jeffrey W.; Kresge, Kristen J.; Pan, Senliang; Cordova, Beverly C.; Klabe, Ronald M.; Rodgers, James D.; Erickson-Viitanen, Susan K. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 3 p. 309 - 312

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Citation Number: 18

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 ...