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

Article

Last updated: 22 Jan 2023

OverviewSimilar Items

Subjects

-

Tags

Pharmaceutical Chemistry

Abstract

Alzheimer's disease (AD) is one of the most prevalent neurodegenerative disorder. 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'-methyl-3', 4'-dihydro1'H-spiro[cyclopentane-1, 2'-quinazoline] (4) in 73.3% yield. The structure of compound 4 was confirmed with GC-MS, 1H and 13C-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.

DOI

10.21608/ejchem.2020.27985.2588

Keywords

Acetylcholine esterase inhibitor, Alzheimer disease, Quinazoline derivatives, Spiro compounds, Molecular docking

Authors

First Name

Rawan

Last Name

Alsuhaimat

MiddleName

A.

Affiliation

Faculty of Pharmacy, Mu’tah University, Al-Karak, 61166, Amman, Jordan

Email

alsuhaimatr@gmail.com

City

-

Orcid

-

First Name

Qais

Last Name

Abualassal

MiddleName

-

Affiliation

Department of Applied Pharmaceutical Sciences, Faculty of Pharmacy, Isra University, Amman, Jordan

Email

qais.abualasal@iu.edu.jo

City

-

Orcid

-

First Name

zead

Last Name

abudyah

MiddleName

-

Affiliation

Faculty of pharmacy / AL-isra university Amman / Jordan

Email

zead.helmi@outlook.com

City

Amman

Orcid

-

First Name

Sherif

Last Name

Ebada

MiddleName

S.

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mu’tah University, Al-Karak, Jordan. and Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University, Cairo, Egypt

Email

sherif_elsayed@pharma.asu.edu.eg

City

-

Orcid

-

First Name

Amgad

Last Name

Albohy

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt (BUE), Egypt

Email

albohy@ualberta.ca

City

-

Orcid

0000-0003-3021-8767

Volume

63

Article Issue

12

Related Issue

18901

Issue Date

2020-12-01

Receive Date

2020-04-15

Publish Date

2020-12-01

Page Start

4,797

Page End

4,804

Print ISSN

0449-2285

Online ISSN

2357-0245

Article File

EJCHEM_Volume 63_Issue 12_Pages 4797-4804.pdf

PDF . 1.4MB

Link

https://ejchem.journals.ekb.eg/article_96061.html

Detail API

https://ejchem.journals.ekb.eg/service?article_code=96061

Order

13

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

https://ejchem.journals.ekb.eg/

MainTitle

-

Details

Type

Article

Created At

22 Jan 2023