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Benzofuran derivatives as ET A-selective, non-peptide endothelin antagonists

…, S Klutchko, EE Reynolds, KM Welch, MA Flynn…

文献索引:Kaltenbronn; Quin III; Reisdorph; Klutchko; Reynolds; Welch; Flynn; Doherty European Journal of Medicinal Chemistry, 1997 , vol. 32, # 5 p. 425 - 431

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被引用次数: 17

摘要

The synthesis and SAR relationships of a series of 4-benzyloxy-3-methylbenzofuran-2- carboxylic acids are described. Compounds from this series show 2-to 16-fold selective binding to the ETA receptor in the micromolar range, and two compounds from this series (32 and 40) were demonstrated to exhibit ETA antagonist activity.