2. Academic Validation
  3. Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385

Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385

  • Bioorg Med Chem Lett. 2006 Apr 1;16(7):1788-94. doi: 10.1016/j.bmcl.2006.01.035.
John F Miller 1,  C Webster Andrews,  Michael Brieger,  Eric S Furfine,  Michael R Hale,  Mary H Hanlon,  Richard J Hazen,  Istvan Kaldor,  Ed W McLean,  David Reynolds,  Douglas M Sammond,  Andrew Spaltenstein,  Roger Tung,  Elizabeth M Turner,  Robert X Xu,  Ronald G Sherrill
Affiliations

Affiliation

  • 1 GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA. john.6.miller@gsk.com
PMID: 16458505 DOI: 10.1016/j.bmcl.2006.01.035
Abstract

A novel series of P1 modified HIV Protease Inhibitors was synthesized and evaluated for in vitro Antiviral activity against wild-type virus and protease inhibitor-resistant viruses. Optimization of the P1 moiety resulted in compounds with femtomolar enzyme activities and cellular Antiviral activities in the low nanomolar range culminating in the identification of clinical candidate GW0385.

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