• Title of article

    Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonists

  • Author/Authors

    C. B. Raju ، نويسنده , , Ilya Okun، نويسنده , , Fiona Stavros، نويسنده , , Ming Fai Chan، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 1997
  • Pages
    6
  • From page
    939
  • To page
    944
  • Abstract
    The potential proteolytic instability of the amide bond present in some ETA selective thiophenesulfonamide endothelin antagonists exemplified by TBC-10708 led us to investigate the replacement of this moiety with stable amide bond surrogates such as a trans double bond and an ethylene spacer. The effect of these replacements on the binding affinity is described.
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    1997
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    788682