Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds |
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| Authors: | Spaltenstein A Almond M R Bock W J Cleary D G Furfine E S Hazen R J Kazmierski W M Salituro F G Tung R D Wright L L |
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| Affiliation: | Glaxo Wellcome Inc, NC 27709, USA. as11513@glaxowellcome.com |
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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. |
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