• Title of article

    Development of tryptase inhibitors derived from thalidomide Original Research Article

  • Author/Authors

    Masashi Tetsuhashi، نويسنده , , Minoru Ishikawa، نويسنده , , Mariko Hashimoto، نويسنده , , Yuichi Hashimoto، نويسنده , , Hiroshi Aoyama، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2010
  • Pages
    16
  • From page
    5323
  • To page
    5338
  • Abstract
    A novel series of tryptase inhibitors with a N-phenylphthalimide skeleton structurally derived from thalidomide (1) has been developed. Structure–activity relationship studies led to a potent and selective tryptase inhibitor, 2-(4-cyanophenyl)isoindole-1,3-dione-5-yl 3-(2-aminopyridin-5-yl)propanoate (7), with the IC50 value of 78 nM.
  • Keywords
    Ceramide , Partial atomic charge , MTT viability assay , Inductive effects , Structure–activity relationship , Resonance , Sphingosine-1-phosphate
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Serial Year
    2010
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Record number

    1306733