石杉碱甲结构改造的研究进展

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.

Advances in the Structural Modification of Huperzine A

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 acetylcholinesterase were described.Among the synthetic huperzine A analogues,the bieactivity of some analogues were superior to the natural huperzine A.The study on the structural modification of huperzine A made great progress.