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ID: ALA1795321

Journal: Bioorg Med Chem Lett

Title: Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonists.

Authors: Xia J, Song J, Zhen L, Zhang X, Lei X, Zheng L, Wang Q, Sun H.

Abstract: 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.

CiteXplore: 21652209

DOI: 10.1016/j.bmcl.2011.05.034