Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.

Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors. Research Abstract Details 

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Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors. Abstract Text:

Huan Wen,Chonglan Lin,Ling Que,Hui Ge,Lin Ma,Rihui Cao,Yiqian Wan,Wenlie Peng,Zihou Wang,Huacan Song,

A series of helicid analogues were prepared and evaluated in vitro for the cholinesterase (AChE and BuChE) inhibitory activities via UV spectroscopy. The results indicated that compounds 5, 6d and 8 exhibited potent AChE inhibitory activities with IC(50) values of 0.45+/-0.02muM, 0.49+/-0.02muM, and 0.20+/-0.01muM, respectively. High selectivity for AChE over BuChE was also observed. Kinetic study showed that the mechanism of AChE inhibition of compounds 5, 6d and 8 was all mixed-type.

Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors. Publishing Authors By Initials

H Wen,C Lin,L Que,H Ge,L Ma,R Cao,Y Wan,W Peng,Z Wang,H Song,

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Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: European journal of medicinal chemistry

VOLUME: 43

Page Numbers: 166-73

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ISSN: 0223-5234

DAY: 5

MONTH: 04

YEAR: 2007

Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors. Information

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LANGUAGE: eng

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Grant and Affiliation Information for Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.

AFFILIATION: School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China.

Country: France

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MEDLINETA: Eur J Med Chem

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