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Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists
W W Mederski1, M Osswald, D Dorsch
1Merck KGaA, Preclinical Pharmaceutical Research, Darmstadt, Germany. mederski@merck.de
Bioorganic & Medicinal Chemistry Letters
|March 31, 1999
Abstract:
The discovery, synthesis and structure-activity relationships of a series of novel benzofuro[3,2-b]pyridines as non-selective endothelin ET(A)/ET(B) as well as selective ET(B) receptor antagonists are described. The most potent non-selective inhibitor 7s displayed an IC50 of 21 nM and 41 nM for ET(A) and ET(B) receptors, respectively, whereas 7ee merely showed affinity for the ET(B) receptor (IC50 = 3.6 nM).