亚苯基双（氧基）双[2,2-二甲基戊酸]：提高高密度脂蛋白的药物。

Phenylenebis(oxy)bis[2,2-dimethylpentanoic acid]s: agents that elevate high-density lipoproteins.

作者信息

Sircar I, Hoefle M, Maxwell R E

出版信息

J Med Chem. 1983 Jul;26(7):1020-7. doi: 10.1021/jm00361a015.

Abstract

A series of phenylenebis(oxy)bis[2,2-dimethylpentanoic acid]s have been synthesized and evaluated as potential hypolipidemic agents. Compound 18 (CI-924) was found to be the most potent compound in this series. In rats, compound 18 not only reduced low-density lipoprotein cholesterol but also increased high-density lipoprotein (HDL) cholesterol. Comparative studies in rats indicated 18 produced an equal elevation of HDL cholesterol at one-third of the dose required of gemfibrozil. Structure-activity relationships are discussed.

摘要

一系列亚苯基双（氧）双[2,2-二甲基戊酸]已被合成并作为潜在的降血脂药物进行评估。发现化合物18（CI-924）是该系列中最有效的化合物。在大鼠中，化合物18不仅降低了低密度脂蛋白胆固醇，还增加了高密度脂蛋白（HDL）胆固醇。在大鼠中的比较研究表明，18在吉非贝齐所需剂量的三分之一时能产生相同程度的HDL胆固醇升高。讨论了构效关系。