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本文报道一些甾体酮肟化合物的合成及其在实验动物中的抗着床、抗早孕效果。其中炔诺酮肟(33),醋炔诺酮肟(36),炔诺酮肟三甲硅醚(35),R-2010酮肟(57),R-2323酮肟(65)以及苯丙酸诺龙酮肟对大鼠具有显著的抗早孕作用,炔诺酮肟(33)以及苯丙酸诺龙酮肟(48)对金黄色地鼠也有抗早孕作用。炔诺酮肟(33),醋炔诺酮肟(36),炔诺酮肟三甲硅醚(35)以及R-2323酮肟(65)亦具有很强的抗着床作用。此类化合物的活性分析表明:“非纯孕激素”酮肟,如炔诺酮肟(33)、醋炔诺酮肟(36),R-2323酮肟(65)等具有很强的抗着床、抗早孕作用,而“纯孕激素”酮肟则无效。苯丙酸诺龙酮肟(48)的作用可能有别于“非纯孕激素”酮肟。
This paper reports the synthesis of some steroidal ketoxime compounds and their anti-implantation and anti-pregnancy effects in experimental animals. Norethisterone oxime (36), norethisterone oxime trimethylsilyl ether (35), R-2010 ketoxime (57), R-2323 ketoxime (65) Nandrolone oxime has significant anti-early pregnancy effects in rats, and norethindrone oxime (33) and nandrolone phenylpropionate (48) also have anti-early pregnancy effects on golden hamsters. Norethisterone oxime (33), acetoxynil oxime (36), norethindrone oxime trimethylsilyl ether (35) and R-2323 ketoxime (65) also have strong anti-implantation effects. The activity analysis of these compounds showed that the “non-progesterone” ketoximes such as norethindrone oxime (33), norethindrone acetate (36) and R-2323 ketoxime (65) Bed, anti-pregnancy effect, and “pure progesterone” ketoxime is invalid. The effect of nandrolone phenylpropionate (48) may differ from that of “non-progestin” ketoximes.