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

Mimi L. Quan,Richard E. Olson,David J. Carini,Christopher D. Ellis,Gregory L. Hillyer,George K. Lalka,Jie Liu,Mary K. VanAtten,Andrew T. Chiu,Pancras C. Wong,Ruth R. Wexler,Pieter B.M.W.M. Timmermans

Bioorganic & Medicinal Chemistry Letters（1994）

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摘要

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.

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