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 MoreChina Synchem Technology Co.,Ltd
website:http://www.cnsynchem.com
Contact:+86-0552-4929311
Address:No.217 Daqing Road
xi'an taima biological engineering co., ltd.
Contact:+8615619038117
Address:6 No,keji road xi'an city of china
Shanghai Egoal Chemical Co.,Ltd
Contact:+86-21-50333091
Address:Yangming Garden Square 3,YangGao North Road 1188, Pudong New District, Shanghai
Qingdao Pana-Life Biochem Co.,Ltd.
Contact:86-532-87683902
Address:No.967 Dalao Road, Licang Zone, Qingdao City,Shandong, China 266021
SHANGHAI T&W PHARMACEUTICAL CO., LTD.
website:http://www.trustwe.com
Contact:+86-21-61551611
Address:601, No. 1, 2277 Nong, Zu Chongzhi Road, Zhangjiang Hightech. Park, Pudong
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)