[2-亚甲基坎利酮的合成与反应]

[Synthesis and reactions of 2-methylene-canrenone].

作者信息

Görlitzer K, Moormann P, Pollow K, Schaffrath M

机构信息

Institut für Pharmazeutische Chemie, Technischen Universität Braunschweig.

出版信息

Arch Pharm (Weinheim). 1995 Feb;328(2):149-55. doi: 10.1002/ardp.19953280211.

DOI:10.1002/ardp.19953280211

PMID:7726741

Abstract

Starting from the Mannich salt 1 of the aldosterone antagonist canrenone or from 2-methylene-canrenone (2) the A-ring annulated hetero- and carbocycles 5, 6, 8-13 were prepared. Receptor (estradiol, progesterone, androgen, gluco- and mineralocorticoid) binding studies and competition studies with the serum proteins SHBG and CBG were carried out using the compounds 2, 3, 4b, 5, 6b, 8 and 12. The relative binding affinities with CBG are below 1%, in all other cases lower than 0.01%.

摘要

从醛固酮拮抗剂坎利酮的曼尼希盐1或2-亚甲基-坎利酮（2）出发，制备了A环稠合的杂环和碳环5、6、8 - 13。使用化合物2、3、4b、5、6b、8和12进行了受体（雌二醇、孕酮、雄激素、糖皮质激素和盐皮质激素）结合研究以及与血清蛋白SHBG和CBG的竞争研究。与CBG的相对结合亲和力低于1%，在所有其他情况下低于0.01%。