Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors

…, LT Bacheler, S Diamond, S Jeffrey…

Index: Corbett, Jeffrey W.; Ko, Soo S.; Rodgers, James D.; Gearhart, Lisa A.; Magnus, Nicholas A.; Bacheler, Lee T.; Diamond, Sharon; Jeffrey, Susan; Klabe, Ronald M.; Cordova, Beverly C.; Garber, Sena; Logue, Kelly; Trainor, George L.; Anderson, Paul S.; Erickson-Viitanen, Susan K. Journal of Medicinal Chemistry, 2000 , vol. 43, # 10 p. 2019 - 2030

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Citation Number: 186

Abstract

A series of 4-alkenyl and 4-alkynyl-3, 4-dihydro-4-(trifluoromethyl)-2-(1 H)-quinazolinones were found to be potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) of human immunodeficiency virus type-1 (HIV-1). The 4-alkenyl-3, 4-dihydro-4-(trifluoromethyl)-2-(1 H)- quinazolinones DPC 082 and DPC 083 and the 4-alkynyl-3, 4-dihydro-4-(trifluoromethyl)-2- (1 H)-quinazolinones DPC 961 and DPC 963 were found to exhibit low nanomolar ...