Design, synthesis and evaluation of graftable thrombin inhibitors for the preparation of blood-compatible polymer materials

Claudio Salvagnini, Catherine Michaux, Julie Remiche, Johan Wouters, Paulette Charlier, Jacqueline Marchand-Brynaert

Research output: Contribution to journalArticle

Abstract

Piperazinyl-amide derivatives of N-α-(3-trifluoromethyl- benzenesulfonyl)-L-arginine (1) were synthesized as graftable thrombin inhibitors. The possible disturbance of biological activity due to a variable spacer-arm fixed on the N-4 piperazinyl position was evaluated in vitro, against human a-thrombin, and in blood coagulation assay. Molecular modelling (in silico analysis) and X-ray diffraction studies of thrombin-inhibitor complexes were also performed. The fixation of bioactive molecules on poly(butylene terephthalate) (PBT) and poly(ethylene terephthalate) (PET) membranes was performed by wet chemistry treatment and evaluated by XPS analysis. Surface grafting of inhibitor Id improved the membrane hemocompatibility by reducing blood clot formation on the modified surface.

Original languageEnglish
Pages (from-to)4209-4220
Number of pages12
JournalOrganic and Biomolecular Chemistry
Volume3
Issue number23
DOIs
Publication statusPublished - 7 Dec 2005

Fingerprint Dive into the research topics of 'Design, synthesis and evaluation of graftable thrombin inhibitors for the preparation of blood-compatible polymer materials'. Together they form a unique fingerprint.

  • Cite this