杀精剂硝苯柳胺合成及药效学研究

Synthesis of a new sperm-killing agent, niphensamide and its pharmacodynamics

目的:合成杀精剂硝苯柳胺,并研究其体内外杀精作用。方法:对杀精剂硝苯柳胺的合成路线和工艺条件进行优化,对产品结构进行分析、检测和成本估算。研究其体内外杀精作用和抗妇科感染作用并观察其毒理学。结果:本品合成路线短,工艺简单,收率高,提纯方便,能耗小,成本低,杀精作用强,无不良反应,遗传毒理试验显示其无“三致”作用。结论:本品有望成为一种安全、高效、廉价、方便的新型避孕药和抗妇科感染剂。

Objective: To synthesize niphensamide and study its in vitro and in vivo sperm-killing effect. Methods: Niphensamide was synthesized by use of an optimized process. Its chemical structure was elucidated. The in vitro and in vivo sperm-killing effects of niphensamide as well as its toxicology and anti-infectious activity in gynecology were observed. Results: The synthetic route was simple and had high yield and low cost process. The pharmacodynamic and toxicological data indicated that niphensamide showed highly in vitro and in vivo sperm-killing effect without significant adverse drug reactions and no 'three genicities'was observed. Conclusion:Niphensamide is hopeful to become a safe,highly effective,inexpensive,convenient and new contraceptive with anti-infectious activity.