221177-51-1Relevant articles and documents
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors
Cocuzza, Anthony J.,Chidester, Dennis R.,Cordova, Beverly C.,Klabe, Ronald M.,Jeffrey, Susan,Diamond, Sharon,Weigelt, Carolyn A.,Ko, Soo S.,Bacheler, Lee T.,Erickson-Viitanen, Susan K.,Rodgers, James D.
, p. 1389 - 1392 (2007/10/03)
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.