Design, Synthesis, and Molecular-modeling Study of Aminothienopyridine Analogues of Tacrine for Alzheimer's Disease

被引：14

作者：

Badran, Mohga M. ^{[1
]}

Hakeem, Maha Abdel ^{[1
]}

Abuel-Maaty, Suzan M. ^{[1
]}

El-Malah, Afaf ^{[1
]}

Salam, Rania M. Abdel ^{[2
]}

机构：

[1] Cairo Univ, Dept Organ Pharmaceut Chem, Fac Pharm, Cairo, Egypt

[2] Cairo Univ, Dept Pharmacol & Toxicol, Fac Pharm, Cairo, Egypt

来源：

ARCHIV DER PHARMAZIE | 2010年 / 343卷 / 10期

关键词：

AChE (Acetylcholine esterase); Alzheimer's disease; Docking; Tacrine analogues; Thienopyridines; ACETYLCHOLINESTERASE INHIBITORS; POTENT;

D O I：

10.1002/ardp.200900226

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-Amino-3-cyanothiophenes were successfully condensed with a number of cycloalkanones to afford tacrine analogues in a one-step reaction mediated with Lewis acid. The newly synthesized compounds have been tested for their ability to inhibit acetylcholine esterase (AChE) activity using tacrine as standard drug. Some of the tested compounds showed moderate inhibitory activity in comparison with tacrine, especially compounds 6a which displayed the highest inhibitory activity. Furthermore, molecular-modeling studies were performed in order to rationalize the obtained biological results.

引用

页码：590 / 601

页数：12

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