Discovery of TBC11251, a Potent, Long Acting, Orally Active Endothelin Receptor-A Selective Antagonist 1

C Wu, MF Chan, F Stavros, B Raju, I Okun…

文献索引：Wu, Chengde; Chan, Ming F.; Stavros, Fiona; Raju; Okun, Ilya; Mong, Seymour; Keller, Karin M.; Brock, Tommy; Kogan, Timothy P.; Dixon, Richard A. F. Journal of Medicinal Chemistry, 1997 , vol. 40, # 11 p. 1690 - 1697

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被引用次数: 132

摘要

Previously we reported the discovery of amidothiophenesulfonamides as endothelin receptor-A antagonists with high potency and selectivity. Replacement of an amide group in this class of compounds with an acetyl group maintained the in vitro binding affinity and in vivo activity while providing a compound with oral bioavailability and longer duration of action. The optimal compound discovered during these studies, 15q (TBC11251), binds ...