SYNTHESIS OF NEW 11-BETA-SUBSTITUTED SPIROLACTONE DERIVATIVES - RELATIONSHIP WITH AFFINITY FOR MINERALOCORTICOID AND GLUCOCORTICOID RECEPTORS

被引：23

作者：

CLAIRE, M

FARAJ, H

GRASSY, G

AUMELAS, A

RONDOT, A

AUZOU, G

机构：

[1] FAC PHARM MONTPELLIER, INSERM, U300, 15 AVE CHARLES FLAHAULT, F-34060 MONTPELLIER, FRANCE

[2] CTR HOSP REG & UNIV POINTE A PITRE, INSERM, U359, F-97159 POINTE A PITRE, Guadeloupe, FRANCE

[3] FAC PHARM MONTPELLIER, CTR BIOCHIM STRUCT, F-34060 MONTPELLIER, FRANCE

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 16期

关键词：

D O I：

10.1021/jm00068a018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Various steroidal 17-spirolactones substituted in the 11beta-position were synthesized to study the relationship between the nature of the 11beta-arm and their affinity for cytosolic mineralocorticoid (MR) and glucocorticoid (GR) receptors prepared from adrenalectomized rabbit kidney or liver. One of them, the 11beta-allenyl-3-oxo-19-nor-17-pregna-4,9-diene-21,17-carbolactone derivative, exhibited the same affinity for MR as aldosterone and a 5-fold higher affinity than mespirenone. Its affinity for GR was found to be relatively low. As suggested by molecular modeling, the marked differences in mineralocorticoid receptor binding affinity could be related to the structural features induced by this 11beta-allenic substituent.

引用

页码：2404 / 2407

页数：4