2. Academic Validation
  3. Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds

Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds

  • Bioorg Med Chem Lett. 2000 Jun 5;10(11):1159-62.
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
Affiliations

Affiliation

  • 1 Glaxo Wellcome Inc, NC 27709, USA. as11513@glaxowellcome.com
PMID: 10866371
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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