4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors
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.
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)
5,5-disubstituted-1,5-dihydro-4,1-benzoxazepin-2 (3H)-ones useful as HIV reverse transcriptase inhibitors
The present invention relates to benzoxazepinones of formula I: STR1 or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same and methods of using the same for treating viral infection or as an assay standard or reagent.
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(2008/06/13)
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