Author/Authors :
Marc Nazaré، نويسنده , , Hans Matter، نويسنده , , Otmar Klingler، نويسنده , , Fahad Al-Obeidi، نويسنده , , Herman Schreuder، نويسنده , , Gerhard Zoller، نويسنده , , Jorg Czech، نويسنده , , Martin Lorenz، نويسنده , , Angela Dudda، نويسنده , , Anusch Peyman، نويسنده , , Hans Peter Nestler، نويسنده , , Matthias Urmann، نويسنده , , Armin Bauer، نويسنده , , Volker Laux، نويسنده , , Volkmar Wehner، نويسنده , , David W. Will، نويسنده ,
Abstract :
A series of novel, highly potent, achiral factor Xa inhibitors based on a benzoic acid scaffold and containing a chlorophenethyl moiety directed towards the protease S1 pocket is described. A number of structural features, such as the requirements of the P1, P4 and ester-binding pocket ligands were explored with respect to inhibition of factor Xa. Compound 46 was found to be the most potent compound in a series of antithrombotic secondary assays.
Keywords :
Factor Xa inhibitor.* Corresponding author. Tel.: +49-69-305-5036 , e-mail: david.will@aventis.com , fax: +49-69-331-399
