Hemophilia Research Today is a free monthly online journal that collates and summarizes the latest research about Hemophilia, including details on genetics, causes, symptoms, blood transfusion.

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

De Nanteuil G, Gloanec P, Béguin S, Giesen PL, Hemker HC, Mennecier P, Rupin A, Verbeuren TJ

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

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.

Published 17 August 2006 in J Med Chem, 49(17): 5047-50.
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