Author/Authors :
Jeffrey W. Corbett، نويسنده , , Kristen J. Kresge، نويسنده , , Senliang Pan، نويسنده , , Beverly C. Cordova، نويسنده , , Ronald M. Klabe، نويسنده , , James D. Rodgers III، نويسنده , , Susan K. Erickson-Viitanen، نويسنده ,
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.