Enamino-oxindole HIV protease inhibitors.

Michael Eissenstat, Tanya Guerassina, Sergei Gulnik, Elena Afonina, Abelardo M Silva, Douglas Ludtke, Hiroko Yokoe, Betty Yu, John Erickson

Sequoia Pharmaceuticals, Inc., Gaithersburg, MD 10878, USA. eissenst@comcast.net

Bioorganic & medicinal chemistry letters 2012 Aug 1

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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. Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Michael Eissenstat, Tanya Guerassina, Sergei Gulnik, Elena Afonina, Abelardo M Silva, Douglas Ludtke, Hiroko Yokoe, Betty Yu, John Erickson. Enamino-oxindole HIV protease inhibitors. Bioorganic & medicinal chemistry letters. 2012 Aug 1;22(15):5078-83