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Synthesis and evaluation of a small library of graftable thrombin inhibitors derived from (L)-arginine.

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 Chem

journal_title

European journal of medicinal chemistry

authors

Salvagnini C,Gharbi S,Boxus T,Marchand-Brynaert J

doi

10.1016/j.ejmech.2006.07.010

subject

Has Abstract

pub_date

2007-01-01 00:00:00

pages

37-53

issue

1

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(06)00282-0

journal_volume

42

pub_type

杂志文章

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