194597-88-1Relevant academic research and scientific papers
Novel inhibitors of HIV protease: Design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds
Spaltenstein, Andrew,Almond, Merrick R.,Bock, William J.,Cleary, Darryl G.,Furfine, Eric S.,Hazen, Richard J.,Kazmierski, Wieslaw M.,Salituro, Francesco G.,Tung, Roger D.,Wright, Lois L.
, p. 1159 - 1162 (2000)
A novel series of HIV protease inhibitors containing cyclic P1/P2 scaffolds has been synthesized and evaluated for biological activity. The trans 3,5-dibenzyl-2-oxo pyrrolidinone ring system resulted in a 50 pM enzyme inhibitor against HIV protease in vitro when combined with an indanolamine derived P'-backbone. This compound also shows comparable activity to currently marketed drugs in the MT-4 cell-based antiviral assay. (C) 2000 Elsevier Science Ltd. All rights reserved.
