低聚胺的血小板聚集抑制和抗凝作用，XIX：4,4'-亚苯基双-sydnone亚胺

Platelet aggregation inhibiting and anticoagulant effects of oligoamines, XIX: 4,4'-Phenylene-bis-sydnone imines.

作者信息

Rehse K, Kämpfe M, Martens A

机构信息

Institut für Pharmazie der Freien Universität Berlin, Germany.

出版信息

Arch Pharm (Weinheim). 1993 Mar;326(3):163-6. doi: 10.1002/ardp.19933260309.

DOI:10.1002/ardp.19933260309

PMID:8481095

Abstract

Fourteen 4,4'-m-phenylene- and two 4,4'-p-phenylene-bis-sydnone imine hydrochlorides have been synthesized. All compounds exhibited good solubility in water. In the m-series the 3-(3-phenylpropyl)-derivative 5c and the 3-hexyl compound 5l showed antiplatelet activities at or below 10 mumol/L (IC50, Born-test with collagen). The corresponding p-compounds had the same (6l) or slightly lower (6c) activity. No effect on the fibrin formation (Quick-test) could be observed.

摘要

已合成了十四种4,4'-间亚苯基双-3-亚甲基-4,5-二氢-1,2,3-恶二唑盐酸盐和两种4,4'-对亚苯基双-3-亚甲基-4,5-二氢-1,2,3-恶二唑盐酸盐。所有化合物在水中均表现出良好的溶解性。在间位系列中，3-(3-苯丙基)衍生物5c和3-己基化合物5l在10 μmol/L及以下浓度时表现出抗血小板活性（IC50，胶原诱导的血小板聚集试验）。相应的对位化合物具有相同（6l）或稍低（6c）的活性。未观察到对纤维蛋白形成（Quick试验）的影响。