非甾体抗生育药物的研究 Ⅱ.对-羟基苯丙烯酸衍生物的合成及其抗生育活性

Studies On the Non-Steroidal Antifertility Agents Ⅱ.Synthesis and antifertility activity of some p-coumaric acid derivatives

摘要: 据报道,对-羟基本丙烯酸(Ⅰ)对小鼠有很好的抗生育作用。鉴于芳基取代的苯乙烯美化合物亦有不同程度的抗生育活性,我们在对-羟基苯丙烯酸的α位,用芳基取代,合成了24个衍生物。初步药理筛选结果表明,化合物Ⅱ_(1,3,7,23)对小鼠有抗早孕作用(P<0.05～0.001),其中以化合物Ⅱ_1为显著(P<0.001)。

Abstract: It was reported that p-coumaric acid (Ⅰ) exerted excellent interceptive activity in pregnant mice, and based on the fact that some aryl substituted styrenes also showed certain extent of antifertility effect, thus twenty four derivatives of α-phenyl or naphthyl p-coumaric acid (Ⅱ1-24) were synthesized for evaluation of their antifertility activity. According to preliminary pharmacological test, four compounds Ⅱ_(1,3,7,23) exhibited significant effects on termination of early pregnancy in mice at the single oral dose of 50mg/kg of body wt/day(P<0.05～0.001),among them, compound Ⅱ_1 was most active (P<0.001).