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Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.
A Spaltenstein
1 ,
M R Almond ,
W J Bock ,
D G Cleary ,
E S Furfine ,
R J Hazen ,
W M Kazmierski ,
F G Salituro ,
R D Tung ,
L L Wright
Jun 05 2000
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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.