2-aryloxycarbonylthiophene-3-sulfonamides highly potent and ET(A) selective endothelin receptor antagonists

Article abstract of DOI:10.1016/S0960-894X(97)00367-3

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.