114322-14-4Relevant articles and documents
A convenient synthesis of novel 3-(heterocyclylsulfonyl)propanoic acids and their amide derivatives
Dorogov, Mikhail V.,Filimonov, Sergey I.,Kobylinsky, Dmitry B.,Ivanovsky, Sergey A.,Korikov, Pavel V.,Soloviev, Mikhail Y.,Khahina, Maria Y.,Shalygina, Elena E.,Kravchenko, Dmitry V.,Ivachtchenko, Alexandre V.
, p. 2999 - 3004 (2007/10/03)
A large number of novel 3-(heterocyclylsulfonyl)propanoic acids and their amide derivatives were prepared in good yields and excellent purity starting from the corresponding heterocyclic compounds. At first, chlorosulfonates were generated by reaction of initial heterocycles with various sulfonating and chlorinating agents followed by their conversion into sodium sulfinates. Treatment of sulfinates with acrylic acid smoothly afforded a series of sulfonylpropionates, which were used as convenient reagents for the preparation of a large number of the corresponding carboxamide derivatives.
SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE
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, (2010/12/01)
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.
