ORF 9371衍生物的合成及其抗着床抗早孕活性筛选  

SYNTHESIS AND BIOLOGICAL EVALUATION OF ORF 9371 AND ITS DERIVATIVES

作　　者：姚军[1] 丁惟培[1] 王菊英[1] 石建平[1] 常翠芳[1] 

机构地区：[1]同济医科大学计划生育研究所

出　　处：《中国药物化学杂志》1990年第1期77-79,共3页Chinese Journal of Medicinal Chemistry

摘　　要：甾体口服避孕药发展到今天,人们已把注意力集中在具有抗着床抗早孕而且雌激素活性较小的新甾体药物,近年来已发现一些有希望的化合物,如Ru 486,RMI 12936,STS 557,ORF 9371,炔诺酮肟等。 ORF 9371(17β-乙酰氧基-17α-孕甾-4-烯-20-炔-3-酮肟,5a),文献报道具有较好的抗着床抗早孕活性,其作用机理可能亦与抗孕酮有关。17β-acetoxyl-17α-pregn-4-en-20-yn-3-one oxime (ORF 9371) and its Δ~4-hydrogenated derivative (5α-dihydro-ORF 9371) were synthesized as follows: First adding acetylene to dehydro-epiandrosteroneand epiandrosterone respectively, then Oppenauer Oxidation to give 3-keto compounds which were then reacted with hydroxylamine to give oximes.By treatting acid anhydrides with ORF 9371 or 5α-dihydro ORF9371, 16 oximes derivatives (including ORF 9371) were prepared and submitted to bioassay for evaluation of their antiimplantation and termination of early pregnancy action. The results showed that the activity of 5α-dihydro ORF 9371 at 5mg/kg in rats was equal to that of ORF 9371 at 10mg/kg. The activity of oxime derivatives showed no significant difference.

关 键 词：ORF 9371 5α-dihydro ORF 9371 antiimplantation  TERMINATION of early pregnancy. 

分 类 号：R914[医药卫生—药物化学]