Synthesis of novel tetrahydro quinazoline-antioxidant hybrid as potential lead compound against Alzheimer's disease

Other Title(s)

تخليق هجين جديد رباعي هيدرو كينازولين مضاد للأكسدة كمركب رصاص محتمل ضد مرض الزهايمر

Dissertant

Ata Allah, Muhammad Khalaf Rashid

Thesis advisor

Abu Diyyah, Ziyad Hilmi

University

Isra University

Faculty

Faculty of Pharmacy

University Country

Jordan

Degree

Master

Degree Date

2022

English Abstract

Alzheimer's disease (AD) has been the most significant public source of mortality within the older people across the world.

It is one of the most prevalent causes of memory loss and cognitive impairment.

It is developed due to a drop in ACh levels that caused damage to cholinergic neurons in the forebrain and hippocampus secondary to an accumulation of oxidative stress mainly ROS and RNS in different brain locations.

Existing treatments for this neurodegenerative illness mainly were symptomatic.

However, several studies discovered that the quinazoline moiety inhibits the AChE enzyme and scavenges free radicals.

To slow the progression of AD, we decided to design and synthesize a new hybrid compound (5) with dual biological functions.

Starting with N-methylisatoic anhydride, a series of steps resulted in the final hybrid molecule (5) characterized by LC-MS, 1H NMR, and 13C NMR.

The pharmacological effect of compound (5) was assessed using the Elman test.

The results of the study showed that compound (5) was co-synthesized (67% yield).

Compound (5) anticholinesterase activity showed significant dose-dependent inhibition of the enzyme by compound 5 (IC50 = 11.89 ϻg / ml, p <0.05) comparable to the galantamine standard (IC50 = 9.570 ϻg / ml).

The synthesis quinazoline-antioxidant derivative (5) has significant inhibitory action and might be used as principal compounds in the development of new AD treatments.

Main Subjects

Pharmacology

No. of Pages

52

Table of Contents

Table of contents.

Abstract.

Abstract in Arabic.

Chapter One : Introduction.

Chapter Two : Literature review.

Chapter Three : Materials and Methodology.

Chapter Four : Chemical synthesis.

Chapter Five : Discussions and Results.

Chapter Six : Conclusions and recommendations.

References.

American Psychological Association (APA)

Ata Allah, Muhammad Khalaf Rashid. (2022). Synthesis of novel tetrahydro quinazoline-antioxidant hybrid as potential lead compound against Alzheimer's disease. (Master's theses Theses and Dissertations Master). Isra University, Jordan
https://search.emarefa.net/detail/BIM-1428677

Modern Language Association (MLA)

Ata Allah, Muhammad Khalaf Rashid. Synthesis of novel tetrahydro quinazoline-antioxidant hybrid as potential lead compound against Alzheimer's disease. (Master's theses Theses and Dissertations Master). Isra University. (2022).
https://search.emarefa.net/detail/BIM-1428677

American Medical Association (AMA)

Ata Allah, Muhammad Khalaf Rashid. (2022). Synthesis of novel tetrahydro quinazoline-antioxidant hybrid as potential lead compound against Alzheimer's disease. (Master's theses Theses and Dissertations Master). Isra University, Jordan
https://search.emarefa.net/detail/BIM-1428677

Language

English

Data Type

Arab Theses

Record ID

BIM-1428677