Synthesis and Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities of 7-Alkoxyl Substituted Indolizinoquinoline-5,12-dione Derivatives

被引：8
|
作者：
Wu, Zu-Ping [1 ]
Wu, Xi-Wei [1 ]
Shen, Ting [1 ]
Li, Yan-Ping [1 ]
Cheng, Xi [1 ]
Gu, Lian-Quan [1 ]
Huang, Zhi-Shu [1 ]
An, Lin-Kun [1 ]
机构：
[1] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
来源：
ARCHIV DER PHARMAZIE | 2012年 / 345卷 / 03期
基金：
中国国家自然科学基金;
关键词：
7-Alkoxyl substituted indolizinoquinoline-5; 12-dione derivatives; Acetylcholinesterase inhibitor; Butyrylcholinesterase inhibitor; Molecular docking study; ALZHEIMERS-DISEASE;
D O I：
10.1002/ardp.201100188
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel 7-alkoxyl substituted indolizinoquinoline-5,12-dione derivatives were synthesized. The cholinesterase inhibition assays indicated that most synthesized compounds exhibited good activity for acetylcholinesterase (AChE) and high selectivity index of AChE over butyrylcholinesterase (BuChE). Compound 12b exhibited the most potent AChE inhibitory activity with an IC50 value of 0.068 mu M and the highest selectivity index of 144. Kinetic study of AChE indicated that a mixed type of inhibition pattern existed for these indolizinoquinoline-5,12-dione derivatives. Molecular docking study indicated that compound 12b could bind to both the catalytically active site and the peripheral anionic site of AChE.
引用
收藏
页码：175 / 184
页数：10
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