1. Academic Validation
  2. Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles

Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles

  • Bioorg Med Chem Lett. 2005 Aug 1;15(15):3496-500. doi: 10.1016/j.bmcl.2005.05.129.
John F Miller 1 Michael Brieger Eric S Furfine Richard J Hazen Istvan Kaldor David Reynolds Ronald G Sherrill Andrew Spaltenstein
Affiliations

Affiliation

  • 1 GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA. john.6.miller@gsk.com
Abstract

A novel series of tyrosine-derived HIV Protease Inhibitors was synthesized and evaluated for in vitro Antiviral activity against wild-type virus and two protease inhibitor-resistant viruses. All of the compounds had wild-type Antiviral activities that were similar to or greater than several currently marketed HIV Protease Inhibitors. In addition, a number of compounds in this series were more potent against the drug-resistant mutant viruses than they were against wild-type virus.

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