周群, 李正化, 郭遂, 吴德光, 余朝菁. A-失碳-5α-雄甾烷化合物的合成及抗生育活性J. 药学学报, 1995, 30(10): 745-751.
引用本文: 周群, 李正化, 郭遂, 吴德光, 余朝菁. A-失碳-5α-雄甾烷化合物的合成及抗生育活性J. 药学学报, 1995, 30(10): 745-751.
Q Zhou, ZH Li, S Guo, DG Wu , CQ Yu, . SYNTHESIS AND ANTIFERTILITY ACTIVITY OF A-NOR-5伪-ANDROSTANE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1995, 30(10): 745-751.
Citation: Q Zhou, ZH Li, S Guo, DG Wu , CQ Yu, . SYNTHESIS AND ANTIFERTILITY ACTIVITY OF A-NOR-5伪-ANDROSTANE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1995, 30(10): 745-751.

A-失碳-5α-雄甾烷化合物的合成及抗生育活性

SYNTHESIS AND ANTIFERTILITY ACTIVITY OF A-NOR-5伪-ANDROSTANE DERIVATIVES

  • 摘要: 设计合成了16个A-失碳-5α-雄甾烷化合物,经红外、核磁、质谱及元素分析等确证结构。小白鼠抗着床试验结果表明化合物8,9,10和16具一定的抗着床活性,2.5mg·kg-1灌胃给药,终止妊娠率67%~75%,其它化合物活性均较低。作者对其可能的构效关系进行了简略的分析。

     

    Abstract: In order to study the relationship between the structure of A-nor-5α-androstanederivatives and their antifertility activity , we designed and synthesized 16 A-nor-5α- androstanecompounds through several reaction steps with dehydroepiandrosterone acetate as a starting material .Their structures were confirmed by IR, 1HNMR ,MS ,elemental analyses ,etc. Preliminary pharmacological tests showed that compounds 8,9,10 and 16 possess antiimplanta-tion activity to some extent(2.5 mg·kr-1 ,administered po, gave 67~75% antiimplantationrate).Other compounds showed low activity. The possible relationship between compound structures and their activities is analysed briefly.

     

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