907185-71-1Relevant articles and documents
Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders
De Nanteuil, Guillaume,Gloanec, Philippe,Béguin, Suzette,Giesen, Peter L. A.,Hemker, H. Coenraad,Mennecier, Philippe,Rupin, Alain,Verbeuren, Tony J.
, p. 5047 - 5050 (2006)
The synthesis and evaluation of inhibitors of activated protein C (aPC) are reported. This serine protease is partly responsible for the degradation of factor Villa, 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.