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-5α-ANDROSTANE DERIVATIVES

作　　者：周群[1] 李正化[1] 郭遂 吴德光 余朝菁 

机构地区：[1]华西医科大学药学院,四川省计划生育科学研究所,上海医科大学药学院有机化学教研室

出　　处：《药学学报》1995年第10期745-751,共7页Acta Pharmaceutica Sinica

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。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.

关 键 词：抗生育活性 失碳雄甾烷 雄甾烷 避孕药 合成 

分 类 号：TQ463.3[化学工程—制药化工] R979.21[医药卫生—药品]