Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.

Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.

Author information

1
F. Hoffmann-La Roche Ltd, CH-4070 Basel, Switzerland. katrin.groebke_zbinden@roche.com

Abstract

Proof of concept experiments have shown that tissue factor/factor VIIa inhibitors have antithrombotic activity without enhancing bleeding propensity. Starting from lead compounds generated by a biased combinatorial approach, phenylglycine amide tissue factor/factor VIIa inhibitors with low nanomolar affinity and good selectivity against other serine proteases of the coagulation cascade were designed, using the guidance of X-ray structural analysis and molecular modelling.

PMID:
15664864
DOI:
10.1016/j.bmcl.2004.10.092
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center