Chemical and Pharmaceutical Bulletin p. 1841 - 1849 (1994)
Update date:2022-08-03
Topics:
Ueyama
Yanagisawa
Kawai
Sonegawa
Baba
Mochizuki
Kosakai
Tomiyama
Substituted pyridines were synthesized as potential angiotensin II (AII) receptor antagonists. Substitution at the position 2 in the pyridine resulted in potent activity, and the optimal alkyl length was four carbons. The potency further increased with the introduction of a hydroxymethyl group at the position 4. One of the compounds, 2-butyl-6-chloro-4-hydroxymethyl-5-methyl-3-[[2'-(1H-tetrazol-5-yl)bip henyl-4-yl]methyl]pyridine 9 h (KT3-579)is a competitive AII antagonist with a pA2 value of 9.31, and is about 10 times more potent than Du Pont 753. It was found to be an AT1 specific antagonist with an IC50 of 3.09 nM.
View MoreSJZ Chenghui Chemical Co., Ltd.
Contact:86-311-87713916
Address:no.368 youyi north avenue
Shanghai Bocimed Pharmaceutical Co., Ltd.
website:http://www.bocimed.com
Contact:+86-21-68861632
Address:Building 1, Lane 647, Songtao Road, Zhangjiang High-Tech Park, Shanghai
Chengdu Pukang Biotechnology Co., Ltd
Contact:+86-28-82550498
Address:No. 558 Rulin Road,Xinjin county,Chengdu city, China
Chengdu NoVi Biotechnology Co., Ltd.(expird)
Contact:13551243286/028-81458053
Address:NO.168-1-224 JULONG ROAD WUHOU DISTRICT, CHENGDU CITY,SICHUAN PROVINCE
Zhejiang kehong chemical co., ltd
Contact:0086-575-85522000
Address:xiner center RD binhai industrial zone shaoxing zhejiang province P.R.China,312073
Doi:10.1016/j.tetlet.2014.11.139
(2015)Doi:10.1002/jlcr.1105
(2006)Doi:10.1021/ja00130a003
(1995)Doi:10.1021/ol990629a
(1999)Doi:10.1248/cpb.45.1860
(1997)Doi:10.1016/0040-4039(95)01114-W
(1995)
