Author/Authors :
Anthony J. Cocuzza، نويسنده , , Dennis R. Chidester، نويسنده , , Beverly C. Cordova، نويسنده , , Ronald M. Klabe، نويسنده , , Susan Jeffrey، نويسنده , , Sharon Diamond، نويسنده , , Carolyn A. Weigelt، نويسنده , , Soo S. Ko، نويسنده , , Lee T. Bacheler، نويسنده , , Susan K. Erickson-Viitanen، نويسنده , , James D. Rodgers III، نويسنده ,
Abstract :
A series of 4,1-benzoxazepinone analogues of efavirenz (Sustiva™) as potent NNRTIs has been discovered. The cis-3-alkylbenzoxazepinones are more potent then the trans isomers and can be synthesized preferentially by a novel stereoselective cyclization. The best compounds are potent orally bioavailable inhibitors of both wild-type HIV-1 and its clinically relevant K103N mutant virus, but are highly protein-bound in human plasma.
