作为降血脂和抗氧化剂的一氧化氮释放吗啉衍生物。

Nitric oxide releasing morpholine derivatives as hypolipidemic and antioxidant agents.

作者信息

Chrysselis Michael C, Rekka Eleni A, Siskou Ioanna C, Kourounakis Panos N

机构信息

Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Thessaloniki 54 124, Greece.

出版信息

J Med Chem. 2002 Nov 21;45(24):5406-9. doi: 10.1021/jm011062i.

DOI:10.1021/jm011062i

PMID:12431068

Abstract

The synthesis and evaluation of activity of some nitric acid esters of substituted morpholines are presented. All compounds inhibit lipid peroxidation and reduce cholesterol (20-63%) and triglyceride (37-85%) plasma levels. The more potent NO donors 14 and 17 specifically reduce low-density lipoprotein (LDL). These data indicate that proper structural modifications to the hypolipidemic and antioxidant morpholines enabling NO production, besides preserving or enhancing the above activities, offer a remarkable reduction of LDL, considered advantageous for antiatheromatic agents.

摘要

本文介绍了一些取代吗啉硝酸酯的合成及其活性评估。所有化合物均能抑制脂质过氧化，并降低血浆胆固醇（20 - 63%）和甘油三酯（37 - 85%）水平。更有效的一氧化氮供体14和17能特异性降低低密度脂蛋白（LDL）。这些数据表明，对具有降血脂和抗氧化作用的吗啉进行适当的结构修饰以产生一氧化氮，除了保留或增强上述活性外，还能显著降低低密度脂蛋白，这对于抗动脉粥样硬化药物来说是有利的。