N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(3- methoxy-5-methylpyrazin-2-ylsulfamoyl)benzamide; one of a class of novel benzenesulphonamides which are orally-active, ET(A)-seIective endothelin antagonists

Article abstract of DOI:10.1016/S0960-894X(97)00228-X

A series of novel sulphonamides have been discovered which show high affinity and selectivity for the endothelin ET(A) receptor. N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(-3-methoxy-5-methylpyrazin-2 -ylsulfamoyl)benzamide (18) is the most widely investigated compound and is a potent antagonist in vivo when dosed either i.v. or orally, and has prolonged oral duration of action.