Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonists
摘要:
A series of novel 2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3,3-diphenyl butyric acid derivatives were synthesized and evaluated for their antagonistic activity for endothelin-1-induced contraction in rabbit aorta. Within this series of compounds, 2-[(4,6-dimethylpyrimidin-2-yl) oxy]-3-cyano-3,3-diphenylpropionic acid (4) displays comparable potency with ambrisentan (1), and warrants further investigation. (C) 2011 Elsevier Ltd. All rights reserved.
Ramart; Amagat, Annales de Chimie (Cachan, France), 1927, vol. <10> 8, p. 295
作者:Ramart、Amagat
DOI:——
日期:——
Ramart; Amagat, Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1924, vol. 179, p. 900
作者:Ramart、Amagat
DOI:——
日期:——
Alkali metal reductions of epoxides, ketals, and related heterocycles. Intermediacy of carbanions
作者:Edwin M. Kaiser、Charles G. Edmonds、Stephen D. Grubb、James W. Smith、Donna Tramp
DOI:10.1021/jo00801a019
日期:1971.1
Bergmann; Weiss, Chemische Berichte, 1930, vol. 63, p. 1173,1175
作者:Bergmann、Weiss
DOI:——
日期:——
Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonists
作者:Jun Xia、Jianfei Song、Le Zhen、Xiuling Zhang、Xiantao Lei、Lina Zheng、Qiujuan Wang、Hongbin Sun
DOI:10.1016/j.bmcl.2011.05.034
日期:2011.7
A series of novel 2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3,3-diphenyl butyric acid derivatives were synthesized and evaluated for their antagonistic activity for endothelin-1-induced contraction in rabbit aorta. Within this series of compounds, 2-[(4,6-dimethylpyrimidin-2-yl) oxy]-3-cyano-3,3-diphenylpropionic acid (4) displays comparable potency with ambrisentan (1), and warrants further investigation. (C) 2011 Elsevier Ltd. All rights reserved.