石杉碱甲结构改造的研究进展  

Advances in the Structural Modification of Huperzine A

作　　者：易家宝[1] 颜杰[1] 李旭明[1] 

机构地区：[1]四川理工学院,自贡643000

出　　处：《天然产物研究与开发》2009年第6期1080-1083,987,共5页Natural Product Research and Development

摘　　要：石杉碱甲是高效、高选择性的可逆性乙酰胆碱酯酶抑制剂,是治疗早老性痴呆症的一个有前景的药物。本文概述了石杉碱甲的性质、结构和构效关系,从结构简化、C10、吡啶酮环、脂桥环、环外双键和桥头氨基等方面综述了石杉碱甲结构改造的研究进展,并描述了所得的新型石杉碱甲类似物的抗乙酰胆碱酯酶的生物活性。在已合成的大量的石杉碱甲类似物中,部分类似物的活性优于天然石杉碱甲,石杉碱甲结构改造的研究取得了可喜的进展。Huperzine A was a powerful selective reversible inhibitor of acetylcholinesterase and a promising drug for Alzheimer＇ s Disease. The property, structure, and structure activity relationship of huperzine A were summarized. The advances in the structural modification of huperzine A were reviewed from the aspects of structure simplification, C10, pyridone ring, fatty bridge ring, double bonds of external ring , amino of bridgehead and so on. And the inhibitory activity of these novel huperzine A analogues against aeetylcholinesterase were described. Among the synthetic huperzine A analogues, the bioactivity of some analogues were superior to the natural huperzine A. The study on the structural modification of huperzine A made great progress.

关 键 词：石杉碱甲类似物 构效关系 结构改造 

分 类 号：R284[医药卫生—中药学] Q946.91[医药卫生—中医学]