• Title of article

    Interaction with the S1β-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors

  • Author/Authors

    Michael D. Wendt، نويسنده , , Andrew Geyer، نويسنده , , William J. McClellan، نويسنده , , Todd W. Rockway، نويسنده , , Moshe Weitzberg، نويسنده , , Xumiao Zhao، نويسنده , , Robert Mantei، نويسنده , , Kent Stewart، نويسنده , , Vicki Nienaber، نويسنده , , Vered Klinghofer، نويسنده , , Vincent L. Giranda، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2004
  • Pages
    6
  • From page
    3063
  • To page
    3068
  • Abstract
    Several 8-substituted 2-naphthamidine-based inhibitors of the serine protease urokinase plasminogen activator (uPA) are described. Direct attachment of five-membered saturated or unsaturated rings improved inhibitor performance; substitution with sulfones further improved binding profiles. Combination of these substituents or of previously described NH-linked heteroaromatic rings with 6-phenyl amide substituents provided further enhancements to potency and selectivity.
  • Keywords
    fax: +1-847-935-5165 , e-mail: mike.d.wendt@abbott.com , Urokinase inhibitors.* Corresponding author. Tel.: +1-847-937-9305
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2004
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    794535