Synthesis and Evaluation of Chroman-4-One Linked to N-Benzyl Pyridinium Derivatives as New Acetylcholinesterase Inhibitors

被引：23

作者：

Arab, Saman ^{[1
,2
]}

Sadat-Ebrahimi, Seyed-Esmail ^{[1
,2
]}

Mohammadi-Khanaposhtani, Maryam ^{[1
,2
]}

Moradi, Alireza ^{[3
]}

Nadri, Hamid ^{[3
]}

Mahdavi, Mohammad ^{[1
,2
]}

Moghimi, Setareh ^{[1
,2
]}

Asadi, Mehdi ^{[1
,2
]}

Firoozpour, Loghman ^{[4
]}

Pirali-Hamedani, Morteza ^{[1
,2
]}

Shafiee, Abbas ^{[1
,2
]}

Foroumadi, Alireza ^{[1
,2
,4
]}

机构：

[1] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran, Iran

[2] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran, Iran

[3] Shahid Sadoughi Univ Med Sci, Fac Pharm, Dept Med Chem, Yazd, Iran

[4] Univ Tehran Med Sci, Drug Design & Dev Res Ctr, Tehran, Iran

来源：

ARCHIV DER PHARMAZIE | 2015年 / 348卷 / 09期

关键词：

Acetylcholinesterase; Alzheimer's disease; Chroman-4-one; Docking study; N-Benzyl pyridinium; BETA-AMYLOID AGGREGATION; ALZHEIMERS-DISEASE; ANTICHOLINESTERASE ACTIVITY; BINDING; DESIGN; CHOLINESTERASES; DOCKING; POTENT;

D O I：

10.1002/ardp.201500149

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of chroman-4-one derivatives containing the N-benzyl pyridinium moiety were designed, synthesized, and evaluated for their acetylcholinesterase (AChE) inhibitory activities. Among the various synthesized compounds, (E)-1-(2,3-dibromobenzyl)-4-((7-ethoxy-4-oxochroman-3-ylidene)methyl)pyridinium bromide (8l) depicted the most potent anti-AChE activity (IC50=0.048M). In addition, the molecular modeling study allowed us to detect possible binding modes that are in full compliance with the observed results through in vitro experiments.

引用

页码：643 / 649

页数：7

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