Seventeen N,N'-benzene-1,3-dimethane and nine N,N',N''-benzene-1,3,5-trimethane derivatives with fluorescent properties have been synthesized. Three of them show antiplatelet activities (inducer collagen, IC50 Born-test) in concentrations < 10 mumol/L. They are suitable for interaction studies with biological macromolecules and synthetical and biological membranes. Structure activity relationships demonstrate that heteropolycyclic fluorophores i.e. quinoline, dibenzofurane, or carbazole are favorable substituents for this purpose.
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Fifteen fluorescent oligoamines with one or two fluorescent groups and two or three basic N-functions were prepared and tested for antiplatelet activity (Born-test). Five compounds involving three different fluorophores, i.e. 2-fluorenyl, 1-pyrenyl, and 9-phenanthryl, show an IC50 of 7-11 mumol/L. They are suitable to serve as probes in the field of oligoamine-biopolymere interactions.
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