| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1382712 | Bioorganic & Medicinal Chemistry Letters | 2016 | 6 Pages |
Abstract
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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Authors
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,