N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.

A series of meta-substituted acetophenone derivatives, encompassing N-(alkyloxycarbonyl)thiophene sulfonamide fragments have been synthesized. Several selective AT2 receptor ligands were identified, among those a tert-butylimidazole derivative (20) with a K of 9.3 nM, that demonstrates a high stability in human liver microsomes (t = 62 min) and in human hepatocytes (t = 194 min).