Title of article
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
4
From page
1159
To page
1162
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790823
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