2. Academic Validation
  3. Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist

Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist

  • Bioorg Med Chem Lett. 2000 Aug 21;10(16):1875-8. doi: 10.1016/s0960-894x(00)00366-8.
Y Kanda 1,  T Takahashi,  Y Araki,  T Konoike,  S Mihara,  M Fujimoto
Affiliations

Affiliation

  • 1 Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan. yasuhiko.kanda@shionogi.co.jp
PMID: 10969989 DOI: 10.1016/s0960-894x(00)00366-8
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 ET(B) selective antagonists. The most potent compound 15f displays IC50 values of 1.7 microM and 0.002 microM to ET(A) and ET(B) receptors, respectively.

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