• Title of article

    Synthesis and biological activity of 1-alkylcarbonylmethyl analogues of YM022

  • Author/Authors

    Graeme Semple، نويسنده , , Hamish Ryder، نويسنده , , David A. Kendrick، نويسنده , , Michael Szelke، نويسنده , , Mitsuaki Ohta، نويسنده , , Masato Satoh، نويسنده , , Akito Nishida، نويسنده , , Shinobu Akuzawa، نويسنده , , Keiji Miyata، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 1996
  • Pages
    4
  • From page
    51
  • To page
    54
  • Abstract
    A novel series of 1-alkylcarbonylmethyl analogues of the potent gastrin/CCK-B receptor antagonist YM022 have been prepared. A number of analogues retained good affinity for the gastrin/CCK-B receptor and one compound (6d) showed improved binding and enhanced selectivity for this receptor over CCK-A. A second compound (6j) gave improved in vivo inhibition of gastric acid secretion in rats. Both analogues were shown to have significantly better activity in the same model following i.d. dosing than either YM022 or L-365,260.
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    1996
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    787855