160232-10-0Relevant academic research and scientific papers
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)
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 18-19, (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.
AMINOPHENYLSULFONAMIDE DERIVATIVES AS HIV PROTEASE INHIBITOR
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Page/Page column 17; 19, (2008/06/13)
The present invention concerns substituted aminophenylsulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broadspectrum 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 and derivatives 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.
Resistance-repellent retroviral protease inhibitors
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Page/Page column 19, (2010/02/14)
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.
Sulfonamide inhibitors of aspartyl protease
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Example 51, (2008/06/13)
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
