• Title of article

    Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: Heterocyclic P3

  • Author/Authors

    David C. Tully، نويسنده , , Hong Liu، نويسنده , , Phil B. Alper، نويسنده , , Arnab K. Chatterjee، نويسنده , , Robert Epple، نويسنده , , Michael J. Roberts، نويسنده , , Jennifer A. Williams، نويسنده , , KhanhLinh T. Nguyen، نويسنده , , David H. Woodmansee، نويسنده , , Christine Tumanut، نويسنده , , Jun Li، نويسنده , , Glen Spraggon، نويسنده , , Jonathan Chang، نويسنده , , Tove Tuntland، نويسنده , , Jennifer L. Harris، نويسنده , , Donald S. Karanewsky، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2006
  • Pages
    6
  • From page
    1975
  • To page
    1980
  • Abstract
    A series of Nα-2-benzoxazolyl-α-amino acid-(arylaminoethyl)amides were identified as potent, selective, and noncovalent inhibitors of cathepsin S. Structure–activity relationships including strategies for modulating the selectivities among cathepsins S, K, and L, and in vivo pharmacokinetics are discussed. A X-ray structure of compound 3 bound to the active site of cathepsin S is also reported.
  • Keywords
    Cathepsin S , cathepsin , Cysteine protease inhibitor , Noncovalent inhibitor , peptidomimetics
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2006
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    796705