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
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.