Rational design, synthesis and biological evaluation of pharmaceutically active cyclohexylquinazoline derivatives

Other Title(s)

التصميم المنطقي و التشييد و التقييم البيولوجي لمشتقات سايكلو هكسيل كوينازولين النشطة صيدلانيا

Dissertant

al-Shish, Asil Nayif Abd al-Munim

Thesis advisor

Abu Diyyah, Zayd

University

Isra University

Faculty

Faculty of Pharmacy

University Country

Jordan

Degree

Master

Degree Date

2021

English Abstract

Alzheimer's disease (AD), the most pervasive form of dementia, remains a universal challenge that must be encountered.

It is considered as a serious neurodegenerative disease which can be extensive enough to results in brain shrinkage and death.

Although the exact cause of AD is still unclear until now, there are different hypothesis regarding its pathogenesis including beta-amyloid (Aβ), cholinergic hypothesis, oxidative stress and others.

Cholinesterase inhibitors was highlighted to be used against Alzheimer's to inhibit the action of acetylcholinesterase enzyme, which is responsible for breaks down acetylcholine neurotransmitter in the brain tissues.

In addition, according to amyloid hypothesis acetylcholinesterase has also non-cholinergic functions that involve stimulation of β-amyloid accumulation.

In this context, different studies have been done on quinazoline hybrids, the promising candidate for AD therapy, for its ability to inhibit acetylcholinesterase (AChE) enzyme and to scavenge excessive amounts of free radicals.

As a part of an ongoing effort toward identifying potent anti‐ Alzheimer's agents, we decided to synthesis and study biologically active novel quinazoline derivatives.

Compounds 3,4 and 5 has been successfully synthesized in good yields (64%,92.6% and 67%), respectively.

An efficient biological evaluation of these compounds for their activity as an acetylcholinesterase inhibitor using Ellman’s method was reported.

The results showed that compound 3 gave the best IC50 value (13.008 ± 0.43µg/ml) which indicated the most potent one as anticholinesterase inhibitor.

All reactions were followed using TLC and characterized their final product using GC-MS, LCMS, ˡH-NMR and ˡ³C-NMR.

Main Subjects

Pharmacology

No. of Pages

45

Table of Contents

Table of contents.

Abstract.

Abstract in Arabic.

Chapter One : Introduction.

Chapter Two : Review articles.

Chapter Three : Materials and method.

Chapter Four : Experimental.

Chapter Five : Results and discussion.

Chapter Six : Conclusions and recommendations.

References.

American Psychological Association (APA)

al-Shish, Asil Nayif Abd al-Munim. (2021). Rational design, synthesis and biological evaluation of pharmaceutically active cyclohexylquinazoline derivatives. (Master's theses Theses and Dissertations Master). Isra University, Jordan
https://search.emarefa.net/detail/BIM-1353044

Modern Language Association (MLA)

al-Shish, Asil Nayif Abd al-Munim. Rational design, synthesis and biological evaluation of pharmaceutically active cyclohexylquinazoline derivatives. (Master's theses Theses and Dissertations Master). Isra University. (2021).
https://search.emarefa.net/detail/BIM-1353044

American Medical Association (AMA)

al-Shish, Asil Nayif Abd al-Munim. (2021). Rational design, synthesis and biological evaluation of pharmaceutically active cyclohexylquinazoline derivatives. (Master's theses Theses and Dissertations Master). Isra University, Jordan
https://search.emarefa.net/detail/BIM-1353044

Language

English

Data Type

Arab Theses

Record ID

BIM-1353044