Asymmetric Synthesis and Biological Evaluation of Cholinesterase Inhibitor Rivastigmine and Analogues Thereof

被引：0

作者：

Xu, Gang ^{[1
]}

Wen, Fuhua ^{[1
]}

Mai, Xiaopang ^{[1
]}

Sun, Pinghua ^{[1
]}

Huang, Meiyan ^{[1
]}

Chen, Weimin ^{[1
]}

机构：

[1] Jinan Univ, Coll Pharm, Guangzhou 510632, Guangdong, Peoples R China

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2010年 / 30卷 / 08期

关键词：

asymmetric synthesis; cholinesterase inhibitor; rivastigmine; analogue; ALZHEIMERS-DISEASE; ACETYLCHOLINESTERASE; DESIGN; THERAPY; ACHE;

D O I：

暂无

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

(S)-Rivastigmine and twelve chiral analogues were synthesized starting from p-hydroxybenzaldehyde or m-hydroxybenzaldehyde via (R)- or (S)-tert-butanesulfinylimines as a chiral initiator, and characterized by IR, H-1 NMR, C-13 NMR and HRMS techniques. Ellman's method was applied to evaluate their bioactivities. Results showed that these compounds exhibited potent inhibitory activities of acetylcholinesterase and butyrylcholinesterase, some of them even superior to rivastigmine.

引用

页码：1185 / 1191

页数：7

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