Benzofuro [3, 2-b] pyridines as mixed ETAETB and selective ET B endothelin receptor antagonists
…, D Dorsch, M Christadler, CJ Schmitges, C Wilm
Index: Mederski, Werner W. K. R.; Osswald, Mathias; Dorsch, Dieter; Christadler, Maria; Schmitges, Claus-Jochen; Wilm, Claudia Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 4 p. 619 - 622
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Citation Number: 28
Abstract
The discovery, synthesis and structure-activity relationships of a series of novel benzofuro [3, 2-b] pyridines as non-selective endothelin ET AET B as well as selective ETB receptor antagonists are described. The most potent non-selective inhibitor 7s displayed an IC50 of 21 nM and 41 nM for ETA and ETB receptors, respectively, whereas 7ee merely showed affinity for the ETB receptor (IC50= 3.6 nM).
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