Nickisch K, Bittler D, Laurent H, Losert W, Casals-Stenzel J, Nishino Y, Schillinger E, Wiechert R
J Med Chem. 1987 Aug;30(8):1403-9. doi: 10.1021/jm00391a023.
Some 15,16-methylene derivatives of the aldosterone antagonist spironolactone were synthesized with the purpose of increasing the antialdosterone potency and reducing the endocrinological effects of this standard compound. By introduction of a 1,2-double bond and a 15 beta,16 beta-methylene ring in the spironolactone molecule both goals were achieved. In animal studies mespirenone exhibited a threefold-greater antialdosterone potency and less than 10% of the antiandrogenic activity of spironolactone.
为提高醛固酮拮抗剂螺内酯的抗醛固酮效力并降低该标准化合物的内分泌效应，合成了约15种15,16-亚甲基衍生物。通过在螺内酯分子中引入1,2-双键和15β,16β-亚甲基环，两个目标均得以实现。在动物研究中，美螺酮的抗醛固酮效力提高了两倍，且抗雄激素活性不到螺内酯的10%。
