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低聚胺的血小板聚集抑制和抗凝作用,XVIII:具有荧光特性的低聚胺,B部分:分子周边的荧光团

Platelet aggregation inhibiting and anticoagulant effects of oligoamines, XVIII: Oligoamines with fluorescent properties, Part B: Fluorophores in the molecular periphery.

作者信息

Rehse K, Seidel T

机构信息

Institut für Pharmazie, Freien Universität Berlin.

出版信息

Arch Pharm (Weinheim). 1994 Jun;327(6):399-404. doi: 10.1002/ardp.19943270611.

DOI:10.1002/ardp.19943270611
PMID:8048847
Abstract

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.

摘要

已经合成了17种具有荧光特性的N,N'-苯-1,3-二甲烷和9种N,N',N''-苯-1,3,5-三甲烷衍生物。其中三种在浓度<10 μmol/L时表现出抗血小板活性(诱导剂胶原蛋白,IC50博恩试验)。它们适用于与生物大分子以及合成膜和生物膜的相互作用研究。构效关系表明,杂多环荧光团,即喹啉、二苯并呋喃或咔唑,是用于此目的的有利取代基。

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