From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3 |
| |
Authors: | Dönnecke Daniel Schweinitz Andrea Stürzebecher Anne Steinmetzer Peter Schuster Maj Stürzebecher Uta Nicklisch Silke Stürzebecher Jörg Steinmetzer Torsten |
| |
Institution: | Curacyte Discovery GmbH, Winzerlaer Str. 2, D-07745 Jena, Germany. |
| |
Abstract: | Highly potent and selective substrate analogue factor Xa inhibitors were obtained by incorporation of non-basic or modestly basic P1 residues known from the development of thrombin inhibitors. The modification of the P2 and P3 amino acids strongly influenced the selectivity and provided potent dual factor Xa and thrombin inhibitors without affecting the fibrinolytic enzymes. Several inhibitors demonstrated excellent anticoagulant efficacy in standard clotting assays in human plasma. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |