• Title of article

    Discovery of selective and nonpeptidic cathepsin S inhibitors

  • Author/Authors

    Osamu Irie، نويسنده , , Takeru Ehara، نويسنده , , Atsuko Iwasaki، نويسنده , , Fumiaki Yokokawa، نويسنده , , Junichi Sakaki، نويسنده , , Hajime Hirao، نويسنده , , Takanori Kanazawa، نويسنده , , Naoki Teno، نويسنده , , Miyuki Horiuchi، نويسنده , , Ichiro Umemura، نويسنده , , Hiroki Gunji، نويسنده , , Keiichi Masuya، نويسنده , , Yuko Hitomi، نويسنده , , Genji Iwasaki، نويسنده , , Kazuhiko Nonomura، نويسنده , , Keiko Tanabe، نويسنده , , Hiroaki Fukaya، نويسنده , , Takatoshi Kosaka، نويسنده , , Christopher R. Snell، نويسنده , , Allan Hallett، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2008
  • Pages
    4
  • From page
    3959
  • To page
    3962
  • Abstract
    Nonpeptidic, selective, and potent cathepsin S inhibitors were derived from an in-house pyrrolopyrimidine cathepsin K inhibitor by modification of the P2 and P3 moieties. The pyrrolopyrimidine-based inhibitors show nanomolar inhibition of cathepsin S with over 100-fold selectivity against other cysteine proteases, including cathepsin K and L. Some of the inhibitors showed cellular activities in mouse splenocytes as well as oral bioavailabilities in rats.
  • Keywords
    Pyrrolopyrimidine , Cathepsin S inhibitor , cysteine protease , nitrile , Nonpeptidic
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2008
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    799692

    • Link To Document
    https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=799692