184644-72-2Relevant academic research and scientific papers
SITAXENTAN DERIVATIVE
-
Paragraph 0137; 0138; 0139, (2013/08/14)
A compound represented by formula (1-1) or (1-2), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of sitaxentan and has an improved CYP inhibitory effect: wherein R1 is a halogen atom, etc., R2 is a methyl group, etc., R3 is a C1-6 alkyl group, etc., and M is a group represented by: etc.
SUBSTITUTED THIOPHENES
-
Page/Page column 65-66, (2008/12/04)
Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2- thiophenecarboxamides as selective endothelin receptor-A antagonists
Wu, Chengde,Chan, Ming F.,Stavros, Fiona,Raju,Okun, Ilya,Castillo, Rosario S.
, p. 1682 - 1689 (2007/10/03)
We report here that N2-aryl-3-(isoxazolylsulfamoyl)-2- thiophenecarboxamides are potent and selective small molecule ET(A) receptor antagonists. The aryl group was subjected to extensive structural modification. With monosubstitution, the para
2-aryloxycarbonylthiophene-3-sulfonamides highly potent and ET(A) selective endothelin receptor antagonists
Raju,Wu, Chengde,Castillo, Rosario,Okun, Ilya,Stavros, Fiona,Chan, Ming Fai
, p. 2093 - 2098 (2007/10/03)
A series of 2-aryloxycarbonylthiophene-3-sulfonamides were synthesized and evaluated to determine their antagonistic activity at the endothelin receptors. N-(4-chloro-3-methyl-5-isoxazolyl)-2-[(3,4-methylenedioxy) phenoxycarbonyl]thiophene-3-sulfonamide was identified as a highly selective, potent (IC50= 8.3 nM) and low molecular weight nonpeptide antagonist.
