57185-66-7Relevant academic research and scientific papers
Styrylsulfonamides
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Page/Page column 16, (2010/11/24)
The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and the
Synthesis and structure-activity relationships in a series of ethenesulfonamide derivatives, a novel class of endothelin receptor antagonists
Harada, Hironori,Kazami, Jun-Ichi,Watanuki, Susumu,Tsuzuki, Ryuji,Sudoh, Katsumi,Fujimori, Akira,Tokunaga, Tatsuhiro,Tanaka, Akihiro,Tsukamoto, Shin-Ichi,Yanagisawa, Isao
, p. 1593 - 1603 (2007/10/03)
In the previous paper, we described a series of the 2-arylethenesulfonamide derivatives, a novel class of ETA-selective endothelin (ET) receptor antagonists, including the compounds 1a, b. Compound 1a showed excellent oral antagonistic activities and pharmacokinetic profiles, and the monopotassium salt of 1 (YM-598 monopotassium) is in clinical trials. In this paper, we wish to report the investigation of the further details of structure-activity relationships (SARs) of the 2-phenylethenesulfonamide region in 1a. It was found that methyl substitutions at the 2-, 4- and 6-positions of the phenyl group in 1a led to the discovery of the ETA/ETB mixed antagonist (6s) with an IC50 of 2.2 nM for the ETA receptor. We also found that introduction of an ethyl group to the 1-position of the ethenyl group in 1a gave the ETA selective antagonist (6u) with an oral endothelin antagonistic activity in rats.
Potential GABAB Receptor Antagonists. VI. The Synthesis of Saclofen and Other Sulfonic Acid Derivatives
Abbenante, Giovanni,Prager, Rolf H.
, p. 1801 - 1810 (2007/10/02)
Saclofen, 3-amino-2-(4-chlorophenyl)propanesulfonic acid (3), has been synthesized by two routes.Attempts to hyrogenolyse or dehydrate the 2-hydroxy derivative were unsuccessful, however.Radical sulfonation of 3-amino-1-bromo-2-(4-chlorophenyl)propene gav
Hypolipidemic alkenesulfonamides
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, (2008/06/13)
Method for lowering blood liped levels in mammals, using certain derivatives of N-carbamoyl-2-phenylethenesulfonamide, many of which are novel.
