313679-57-1Relevant articles and documents
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: The discovery of GW0385
Miller, John F.,Andrews, C. Webster,Brieger, Michael,Furfine, Eric S.,Hale, Michael R.,Hanlon, Mary H.,Hazen, Richard J.,Kaldor, Istvan,McLean, Ed W.,Reynolds, David,Sammond, Douglas M.,Spaltenstein, Andrew,Tung, Roger,Turner, Elizabeth M.,Xu, Robert X.,Sherrill, Ronald G.
, p. 1788 - 1794 (2007/10/03)
A novel series of P1 modified HIV protease inhibitors was synthesized and evaluated for in vitro antiviral activity against wild-type virus and protease inhibitor-resistant viruses. Optimization of the P1 moiety resulted in compounds with femtomolar enzyme activities and cellular antiviral activities in the low nanomolar range culminating in the identification of clinical candidate GW0385.
Inhibitors of aspartyl protease
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Page 55-56; 64, (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.