873584-07-7Relevant academic research and scientific papers
Synthesis and evaluation of a small library of graftable thrombin inhibitors derived from (l)-arginine
Salvagnini, Claudio,Gharbi, Sonia,Boxus, Thierry,Marchand-Brynaert, Jacqueline
, p. 37 - 53 (2007)
Novel piperazinyl-amide derivatives of N-α-(aryl-sulfonyl)-l-arginine were synthesized as graftable thrombin inhibitors, in the context of biomaterials' design. The possible disturbance of biological activity due to a variable spacer-arm fixed on the N-4 piperazinyl position and the introduction of a trifluoromethyl group as XPS (X-ray Photoelectron Spectroscopy) tag on the sulfonamide moiety were evaluated in vitro against human α-thrombin. All the compounds of the library were found to be active at the micromolar level, as the reference TAME (N-tosyl-l-arginine methyl ester). The blood compatibilization improvement of poly(ethylene terephthalate) (PET) membrane, coated or grafted by wet chemistry treatment with one representative inhibitor of the library, was also evaluated, showing interesting decrease in blood clot formation.
Design, synthesis and evaluation of graftable thrombin inhibitors for the preparation of blood-compatible polymer materials
Salvagnini, Claudio,Michaux, Catherine,Remiche, Julie,Wouters, Johan,Charlier, Paulette,Marchand-Brynaert, Jacqueline
, p. 4209 - 4220 (2007/10/03)
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. The Royal Society of Chemistry 2005.
