Design and synthesis of thienopyridines as novel templates for acetylcholinesterase inhibitors

被引：5

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, Fac Pharm, Dept Organ Pharmaceut Chem, Giza, Egypt

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

来源：

MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 09期

基金：

欧盟地平线“2020”;

关键词：

Synthesis; Thienopyridines; AChE inhibitors; Alzheimer's disease; POTENTIAL INTEREST; TACRINE-HUPERZINE; DERIVATIVES; HYPOTHESIS; LIGANDS; POTENCY; HYBRIDS;

D O I：

10.1007/s00044-012-0403-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New dual binding site acetylcholinesterase (AChE) inhibitors have been designed and synthesized as a new drug candidate for the treatment of Alzheimer's disease (AD) through the binding to both catalytic and peripheral sites of the enzyme. Therefore, a series of thienopyridine analogs of tacrine were synthesized and investigated for their ability to inhibit the activity of AChE in comparison with tacrine. All the compounds were found to inhibit AChE activity, especially compounds 7b and 11a, which were found to be more potent than tacrine.

引用

页码：4087 / 4095

页数：9

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