源自3-羟基-17,17-二甲基孕甾-1,3,5(10),8,11,13-六烯的潜在降血脂药物。

Potential hypolipidemic agents derived from 3-hydroxy-17,17-dimethylgona-1,3,5(10),8,11,13-hexaene.

作者信息

Chinn L J, Salamon K W

出版信息

J Med Chem. 1977 Feb;20(2):229-33. doi: 10.1021/jm00212a008.

Abstract

Numerous aryloxy derivatives containing a lipophilic group have been found to possess hypolipidemic activity. This has prompted the preparation of various derivatives of 3-hydroxy-17,17-dimethylgona-1,3,5(10),8,11,13-hexaene (6a). In 6a the lipophilic biphenyl group is incorporated into the steroid nucleus. A three-step synthesis of 6a from 17beta-methylestradiol methyl ether was developed. The derivatives prepared were tested in rats made hypercholesterolemic with propylthiouracil. Several were found active in this test.

摘要

已发现许多含有亲脂性基团的芳氧基衍生物具有降血脂活性。这促使人们制备了3-羟基-17,17-二甲基-1,3,5(10),8,11,13-六烯孕甾（6a）的各种衍生物。在6a中，亲脂性联苯基被并入甾体核中。开发了一种从17β-甲基雌二醇甲醚三步合成6a的方法。所制备的衍生物在用丙基硫氧嘧啶使其产生高胆固醇血症的大鼠中进行了测试。发现其中几种在该测试中具有活性。