Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonists |
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| Authors: | Xia Jun Song Jianfei Zhen Le Zhang Xiuling Lei Xiantao Zheng Lina Wang Qiujuan Sun Hongbin |
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| Affiliation: | a Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China
b Department of Pharmacology, College of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China |
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| 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. |
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| Keywords: | Endothelin receptor Ambrisentan analogues Pulmonary arterial hypertension SAR analysis Antagonists |
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