摘要
为了探索双炔失碳酯类A-失碳-5α-雄甾烷衍生物的结构与抗生育活性的关系,寻找抗早孕有效的甾体化合物,本文设计合成了7个炔氢被氯原子取代的双炔失碳酯类似物。其结构经元素分析、质谱、红外、核磁共振等确证。小鼠抗早孕试验结果表明,此类化合物的抗早孕活性较双炔失碳酯低。作者对其可能的构效关系进行了分析。
In order to study the relationship between the structtires of A-nor-5α-androstane derivatives and their antifertility activities, and to find new steroids with anti-early pregnant effect,seven anordrin analogues with the ethynyl hydrogen substituted by a chloride were designed and synthesized.Their structures were confirmed by EA,MS,IR,1 ̄HNMR,etc.The anti-early pregnant test on mice showed that,except compound 3),other compounds possessed low anti-early pregnant activity.when 6 mg/kg were administered p.o.,the percentage of pregnant stopping was≤38%.The possible relationship between the structures of the compounds and their antifertility activities was analysed briefly.
出处
《中国药物化学杂志》
CAS
CSCD
1995年第2期86-90,共5页
Chinese Journal of Medicinal Chemistry