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 MoreSuzhou Tianma Specialty Chemicals Co.,Ltd
Contact:+86-512-68090577
Address:#199, Huayuan Rd, Mudu, Suzhou, Jiangsu, CHINA
Contact:18698110882
Address:1303 No2 building,LuoMa Garden,YongAn Road,Hexi District,Tianjin city
Nanjing Habo Medical Technology Co., Ltd.
Contact:025-85769882
Address:No.108. Ganjiabian east. Qixia District .Nanjing
Hubei Xinghuo Chemical Co., Ltd.,
Contact:13925817279 13907299441
Address:Xinghuo Fine Chemistry Industrial Park, Xiaochang County, Hubei Province, China
Cangzhou Senary Chemical Science-tech Co., Ltd
Contact:+86-317-3563899, 3563699
Address:168 Jinde Road, Cangzhou, Hebei, China
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)