Balanced angiotensin II receptor antagonists. I. The effects of biphenyl “ortho”-substitution on AT1/AT2 affinities

Biphenyl “ortho”-substitution of DuP 753-like AT1-selective angiotensin II receptor antagonists provides AT2 affinity. When combined with a sulfonylcarbamate as the acid isostere, balanced AT1/AT2 receptor antagonists were obtained. Some compounds exhibited nanomolar affinities for both receptors and good AT2/AT1 ratios; these compounds also produce potent and prolonged antihypertensive effects in renal hypertensive rats.