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邻苯二甲酰亚胺衍生物的降血脂活性。1. N-取代邻苯二甲酰亚胺衍生物。

Hypolipidemic activity of phthalimide derivatives. 1. N-Substituted phthalimide derivatives.

作者信息

Chapman J M, Cocolas G H, Hall I H

出版信息

J Med Chem. 1979 Nov;22(11):1399-402. doi: 10.1021/jm00197a022.

Abstract

The general lipid-lowering action of the N-substituted phthalimide derivatives reported herein, as well as the activity of potassium phthalimide, implicates the phthalimide moiety as possessing hypolipidemic activity in rodents. Compounds containing substituents with chain lengths of four carbon or oxygen atoms showed the best hypolipidemic activity in the series tested. Tests involving 1-N-phthalimidobutan-3-one demonstrated a dose-dependent hypolipidemic action free of estrogenic side effects, with no apparent deposition of cholesterol in body organs, and with a high therapeutic index. Further work on the hypolipidemic activity of phthalimido, as well as other imido compounds, is underway.

摘要

本文报道的N-取代邻苯二甲酰亚胺衍生物的一般降脂作用,以及邻苯二甲酰亚胺钾的活性,表明邻苯二甲酰亚胺部分在啮齿动物中具有降血脂活性。在测试的系列化合物中,含有四个碳原子或氧原子链长取代基的化合物显示出最佳的降血脂活性。涉及1-N-邻苯二甲酰亚胺基丁-3-酮的试验表明其具有剂量依赖性的降脂作用,无雌激素副作用,体内器官无明显胆固醇沉积,且治疗指数高。关于邻苯二甲酰亚胺以及其他亚胺化合物的降血脂活性的进一步研究正在进行中。

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