Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B

Song Feng; Yu Xia; Dongmei Han; Chunyan Zheng; Xuchang He; Xican Tang; Donglu Bai

doi:10.1016/j.bmcl.2004.11.060

Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B

Bioorg Med Chem Lett. 2005 Feb 1;15(3):523-6. doi: 10.1016/j.bmcl.2004.11.060.

Authors

Song Feng¹, Yu Xia, Dongmei Han, Chunyan Zheng, Xuchang He, Xican Tang, Donglu Bai

Affiliation

¹ State Key Laboratory for New Drug Research, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.

PMID: 15664805
DOI: 10.1016/j.bmcl.2004.11.060

Abstract

By targeting dual active sites of AChE, a number of new derivatives of HupB have been synthesized and tested as acetylcholinesterase inhibitors. The most potent compound, bis-HupB 5b is 72-fold more potent in AChE inhibition and 79-fold more selective for AChE versus BChE than HupB.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Alkaloids / chemical synthesis*
Alkaloids / pharmacology
Animals
Binding Sites
Cerebral Cortex
Cholinesterase Inhibitors / chemical synthesis*
Cholinesterase Inhibitors / pharmacology
Drugs, Chinese Herbal / chemical synthesis
Drugs, Chinese Herbal / pharmacology
Rats
Structure-Activity Relationship

Substances

Alkaloids
Cholinesterase Inhibitors
Drugs, Chinese Herbal
huperzine B