Journal of Medicinal Chemistry p. 2525 - 2547 (1991)
Update date:2022-09-26
Topics:
Carini, David J.
Duncia, John V.
Aldrich, Paul E.
Chiu, Andrew T.
Johnson, Alexander L.
et al.
A new series of nonpeptide angiotensin II (AII) receptor antagonists has been prepared.These N-(biphenylylmethyl)imidazoles, e.g. 2-butyl-1-<(2'-carboxybiphenyl-4-yl)methyl>-4-chloro-5-(hydroxymethyl)imidazole, differ from the previously reported N-(benzamidobenzyl)imidazoles and related compounds in that they produce a potent antihypertensive effect upon oral administration; the earlier series generally were active only when administered intravenously.It has been found that the acidic group at the 2'-position of the biphenyl is essential.Only ortho-substituted acids possess both high affinity for the AII receptor and good oral antihypertensive potency.The carboxylic acid group has been replaced with a variety of acidic isosteres, and the tetrazole ring has been found to be the most effective.The tetrazole derivative, DuP 753, is currently in development for the treatment of hypertension.
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