2. Academic Validation
  3. Enamino-oxindole HIV protease inhibitors

Enamino-oxindole HIV protease inhibitors

  • Bioorg Med Chem Lett. 2012 Aug 1;22(15):5078-83. doi: 10.1016/j.bmcl.2012.05.120.
Michael Eissenstat 1,  Tanya Guerassina,  Sergei Gulnik,  Elena Afonina,  Abelardo M Silva,  Douglas Ludtke,  Hiroko Yokoe,  Betty Yu,  John Erickson
Affiliations

Affiliation

  • 1 Sequoia Pharmaceuticals, Inc., Gaithersburg, MD 10878, USA. eissenst@comcast.net
PMID: 22749283 DOI: 10.1016/j.bmcl.2012.05.120
Abstract

We have designed and synthesized a series of HIV Protease Inhibitors (PIs) with enamino-oxindole substituents optimized to interact with the S2' subsite of the HIV Protease binding pocket. Several of these inhibitors have sub-nanomolar K(i) and Antiviral IC(50) in the low nM range against WT HIV and against a panel of multi-drug resistant (MDR) strains.

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