A series of potent, selective, conformationally restricted angiotensin
II (AII) receptor antagonists has been discovered Two classes of conf
ormationally restricted analogues were prepared: triazolone-based and
imidazole-based biphenyl derivatives. The mast active compound, an imi
dazole-based analogue, has an IC50 of 11 nM and a pA(2) of 8.8.