New N. alpha.-Guanidinobenzoyl Derivatives of Hirudin-54-65 Containing Stabilized Carboxyl or Phosphoryl Groups on the Side Chain of Phenylalanine-63

C Thurieau, S Simonet, J Paladino…

Index: Thurieau, Christophe; Simonet, Serge; Paladino, Joseph; Prost, Jean-Francois; Verbeuren, Tony; Fauchere, Jean-Luc Journal of Medicinal Chemistry, 1994 ,  vol. 37,  # 5  p. 625 - 629

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Citation Number: 13

Abstract

Results The hirudin-C-terminal related analogues were evaluated for their ability to inhibit the a-thrombin-mediated hydrolysis of fibrinogen in vitro (thrombin time). The results are shown in Table 1. All the compounds were found to have micromolar activities as expressed by the concentration of the inhibitor tested that doubled thrombin time. The dessulfated or desphosphorylated analogs