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.
View MoreHangzhou Showland Technology Co., Ltd.
Contact:86-571-88920516
Address:ROOM2118,NO.553,WENSAN ROAD,HANGZHOU,CHINA
Jiangsu Jiuri Chemical Co.,Ltd.
Contact:+86-519-82118868
Address:Tianwang Town, Jurong City, Jiangsu Province, China
Binzhou Holly Pharmaceutical Co.,Ltd.
Contact:74517
Address:No.15 Dapu Road,Huangpu District Shanghai,P.R.China
ShangHai Ruiyi Medical Technology Co.,Ltd.
Contact:+86-21-54718086
Address:No951 Jianchuan RD,Minhang District
Chemsky(shanghai)International Co.,Ltd.
Contact:0
Address:0
Doi:10.1016/j.tet.2011.10.043
(2011)Doi:10.1021/ol203041b
(2011)Doi:10.1016/j.dyepig.2011.07.022
(2012)Doi:10.1039/c1cc14463d
(2011)Doi:10.1248/cpb.39.1038
(1991)Doi:10.1039/c1cc15609h
(2011)