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J Med Chem. 2006 Aug 24;49(17):5047-50.

Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders.

Author information

1
Division D of Medicinal Chemistry and Division of Angiology, Institut de Recherches Servier, 11 Rue des Moulineaux, 92150 Suresnes, France. guillaume.denanteuil@fr.netgrs.com

Abstract

The synthesis and evaluation of inhibitors of activated protein C (aPC) are reported. This serine protease is partly responsible for the degradation of factor VIIIa, involved in the regulation of bleeding in hemophilia A. Benzamidine-containing derivatives were found to be potent aPC inhibitors, some of them showing selectivity against the procoagulant protease thrombin. Moreover, compound 1 significantly restored the generation of thrombin in hemophiliac plasma.

PMID:
16913694
DOI:
10.1021/jm0606950
[Indexed for MEDLINE]

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