865105-52-8Relevant articles and documents
Enamino-oxindole HIV protease inhibitors
Eissenstat, Michael,Guerassina, Tanya,Gulnik, Sergei,Afonina, Elena,Silva, Abelardo M.,Ludtke, Douglas,Yokoe, Hiroko,Yu, Betty,Erickson, John
, p. 5078 - 5083 (2012/09/07)
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 Ki and antiviral IC50 in the low nM range against WT HIV and against a panel of multi-drug resistant (MDR) strains.
SUBSTITUTED AMINOPHENYLSULFONAMIDE COMPOUNDS AS HIV PROTEASE INHIBITOR
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Page/Page column 18-20, (2008/06/13)
The present invention concerns substituted aminophenylsulfonamide compounds, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present substituted aminophenylsulfonamide compounds with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
Resistance-repellent retroviral protease inhibitors
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Page/Page column 27, (2008/06/13)
Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.