Discovery and synthesis of a potent sulfonamide ET B selective antagonist

Y Kanda, T Takahashi, Y Araki, T Konoike…

Index: Kanda, Yasuhiko; Takahashi, Tadashi; Araki, Yoshitaka; Konoike, Toshiro; Mihara, Shin-ichi; Fujimoto, Masafumi Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 16 p. 1875 - 1878

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Citation Number: 7

Abstract

The synthesis and structure–activity relationships of a series of sulfonamide endothelin antagonists are described. In the course of our modification studies, we discovered ETB selective antagonists. The most potent compound 15f displays IC50 values of 1.7 μM and 0.002 μM to ETA and ETB receptors, respectively.