长效避孕制剂：左炔诺孕酮的脂肪族和脂环族羧酸酯

Long-acting contraceptive agents: aliphatic and alicyclic carboxylic esters of levonorgestrel.

作者信息

Shafiee A, Vossoghi M, Savabi F, Watson T G, Schubert K, Ponsold K, Werner W, Wagner H, Vlahov R, Tarpanov V

出版信息

Steroids. 1983 Mar;41(3):349-59. doi: 10.1016/0039-128x(83)90106-x.

PMID:6419408

Abstract

Esters of levonorgestrel (13 beta-ethyl-17 alpha-ethynyl-17 beta-hydroxygon-4-en-3-one) with a variety of aliphatic and alicyclic carboxylic acids have been prepared and characterised. In tests for the suppression of estrus in rats, esters with short-chain aliphatic acids and with cyclobutane-carboxylic acid were considerably more active than the standard, norethisterone enanthate (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one). Such esters show great promise for development as long-acting progestogens.

摘要

已制备并表征了左炔诺孕酮（13β-乙基-17α-乙炔基-17β-羟基-4-烯-3-酮）与多种脂肪族和脂环族羧酸形成的酯。在抑制大鼠发情的试验中，含短链脂肪族酸的酯和含环丁烷羧酸的酯比标准品庚酸炔诺酮（17α-乙炔基-17β-羟基-4-烯-3-酮）活性高得多。这类酯作为长效孕激素显示出巨大的开发前景。