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 ,
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