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, ETA-Selective endothelin antagonists

Abstract 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.