Synthesis and Docking Studies of a Novel Tetrahydroquinazoline Derivative as Promising Scaffold for Acetylcholine Esterase Inhibition

被引：3

作者：

Alsuhaimat, Rawan A. ^{[1
]}

Abualassal, Qais ^{[2
]}

Abudayeh, Zead Helmi ^{[2
]}

Ebada, Sherif S. ^{[1
,3
,4
]}

Albohy, Amgad ^{[5
]}

机构：

[1] Mutah Univ, Dept Pharmaceut Chem, Fac Pharm, Al Karak, Jordan

[2] Isra Univ, Dept Appl Pharmaceut Sci, Fac Pharm, Amman, Jordan

[3] Sinai Univ, Dept Pharmacognosy, Fac Pharm, Ismailia, Egypt

[4] Ain Shams Univ, Dept Pharmacognosy, Fac Pharm, Cairo, Egypt

[5] British Univ Egypt BUE, Dept Pharmaceut Chem, Fac Pharm, Suez Desert Rd, Cairo 11837, Egypt

来源：

EGYPTIAN JOURNAL OF CHEMISTRY | 2020年 / 63卷 / 12期

关键词：

Acetylcholine esterase inhibitor; Alzheimer disease; Quinazoline derivatives; Spiro compounds; Molecular Docking; CHOLINESTERASE-INHIBITORS; ACHE INHIBITORS; POTENT; DISCOVERY;

D O I：

10.21608/EJCHEM.2020.27985.2588

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Alzheimer's disease (AD) is one of the most prevalent neurodegenerative disorders. While pathological hallmarks of this disorder are known, the exact cause of AD remains unclear. Quinazoline was found to be a promising scaffold for the design and development of Acetylcholinesterase (AChE) inhibitors. In this study, we report the synthesis of 1'-methy1-3',4'-dihydro1'H-spiro[cyclopentane-1, 2'-quinazoline] (4) in 73.3% yield. The structure of compound 4 was confirmed with GC-MS, di and C-13-NMR. Acetylcholine esterase inhibition was studied virtually with docking into AChE active site and suggests potential use of 4 as a promising scaffold for acetylcholine esterase inhibitor design which might be useful for Alzheimer's disease.

引用

页码：4797 / 4804

页数：8

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