Ruggieri P D, La Macchia G, Rigamonti G, Sighinolfi O, Villa G
Farmaco Sci. 1976 Dec;31(12):849-55.
The structure-activity relationship of some topically applied 21-desoxy-substituted steroids as anti-inflammatory agents was investigated; the anti-inflammatory activity remained unaltered or increased on introducing a methyl group in position 6alpha and a hydroxyl group in position 11beta, even after eliminating the hydroxyl group in position 21. The activity of the molecule was further increased by the introduction of a hydroxyl group in position 17alpha and a fluorine atom in position 9alpha.
研究了一些局部应用的21-脱氧取代甾体作为抗炎剂的构效关系;即使在去除21位的羟基后,在6α位引入甲基和在11β位引入羟基,其抗炎活性仍保持不变或增强。通过在17α位引入羟基和在9α位引入氟原子,分子的活性进一步提高。