Synthesis and pharmacological study of huperzine A-E2020  combined compound

Acta Chimica Sinica ›› 2000, Vol. 58 ›› Issue (5): 580-587. Previous Articles Next Articles

Original Articles

石杉碱甲-E2020拼合物的合成及药理研究

曾繁星;蒋华良;翟宇峰;刘东祥;章海燕;陈凯先;嵇汝运

中国科学院上海药物研究所.上海(200031)

发布日期:2000-05-15

Synthesis and pharmacological study of huperzine A-E2020 combined compound

Zeng Fanxing;Jiang Hualiang;Di Yufeng;Liu Dongxiang;Zhang Haiyan;Chen Kaixian;Ji Ruyun

Shanghai Inst Mat Med., CAS.Shanghai(200031)

Published:2000-05-15

Abstract

The synthesis of huperzine-E2020 combined compound(1) has been accomplished and the activities of 1 and the intermediates 10 and 11 to inhibit the activity of acetylcholinesterase have been measured. Conformational analyses and molecular docking studies of E2020 and the eight isomers of 10 were carried out. The results indicated that binding energies of all isomers of 10 with TcAChE is much lower than E2020 except for RRZ, which might be the reason that the activity of 10 is lower than that of E2020. Interaction pattern of RRZ in TcAChE was also studied. Both docking studies and binding energy showed that the biological activity of RRZ might be higher than that of E2020.

Key words: LYCOPODIUM SERRATUM THUNB, PHARMACOLOGY, BIOLOGICAL ACTIVITY, ALKALOID, ACETYLCHOLINESTERASE, INHIBITOR

CLC Number:

R96
R914

Cite this article

Zeng Fanxing;Jiang Hualiang;Di Yufeng;Liu Dongxiang;Zhang Haiyan;Chen Kaixian;Ji Ruyun. Synthesis and pharmacological study of huperzine A-E2020 combined compound[J]. Acta Chimica Sinica, 2000, 58(5): 580-587.

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石杉碱甲-E2020拼合物的合成及药理研究

Synthesis and pharmacological study of huperzine A-E2020 combined compound

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