Nickisch K, Beier S, Bittler D, Elger W, Laurent H, Losert W, Nishino Y, Schillinger E, Wiechert R
Research Laboratories, Schering AG Berlin and Bergkamen, Berlin, Germany.
J Med Chem. 1991 Aug;34(8):2464-8. doi: 10.1021/jm00112a022.
Several steroidal 6,6-ethylene-15,16-methylene 17-spirolactones were synthesized to find new progestogens that exhibit both progestational and antimineralocorticoidal activities. The influence of substituents in the 10- and 13-position of the steroidal framework on both properties was investigated. It was found that only compound 12, carrying methyl groups at the 10- and 13-positions, possesses high progestational and antimineralocorticoidal activity.
合成了几种甾体6,6-亚乙基-15,16-亚甲基-17-螺内酯,以寻找兼具孕激素活性和抗盐皮质激素活性的新型孕激素。研究了甾体骨架10位和13位取代基对这两种性质的影响。发现只有在10位和13位带有甲基的化合物12具有高孕激素活性和抗盐皮质激素活性。