Abstract:
:Novel piperazinyl-amide derivatives of N-alpha-(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 alpha-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.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Salvagnini C,Gharbi S,Boxus T,Marchand-Brynaert Jdoi
10.1016/j.ejmech.2006.07.010subject
Has Abstractpub_date
2007-01-01 00:00:00pages
37-53issue
1eissn
0223-5234issn
1768-3254pii
S0223-5234(06)00282-0journal_volume
42pub_type
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