抗着床药物的研究——Ⅰ.三氟甲基三苯乙烯类衍生物的合成

STUDIES ON ANTIIMPLANTATION DRUGS——Ⅰ. SYNTHESIS OF SOME TRIFLUOROMETHYL TRIPHENYLETHYLENE DERIVATIVES

摘要: 本文报道合成了具有不同取代基的三氟甲基三苯乙烯类化合物以及Ⅰ_b的氢化产物Ⅱ,并试验其抗着床作用。经初步药理试验发现Ⅰ_b(R=OCH₃)与Ⅰ_c(R=OC₂H₅)作用最强,大白鼠口服给药0.03mg/kg,连续三天,有显著抗生育作用。

Abstract: A series of substituted 1-trifluoromethyl-triphenylethyleneand Ⅰ-trifluoromethyl-Ⅰ, 2-diphenyl-2p-methoxy-phenylethane were synthesized. Among these the most potent compounds were Ⅰ_b(R=—OCH₃)and Ⅰ_c(R=—OC₂H₅), both afforded marked antifertility activity in female rats when given orally at a dose of 0.030 mg/kg per day for three consecutive days.