Author/Authors :
Andrew Spaltenstein، نويسنده , , Merrick R. Almond، نويسنده , , William J. Bock، نويسنده , , Darryl G. Cleary، نويسنده , , Eric S. Furfine، نويسنده , , Richard J. Hazen، نويسنده , , Wieslaw M. Kazmierski، نويسنده , , Francesco G. Salituro، نويسنده , , Roger D. Tung، نويسنده , , Lois L. Wright، نويسنده ,
Abstract :
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.
