Design and synthesis of a potential lead compound quinazoline-lipoic acid derivative for the treatment of Alzheimer’s disease

Other Title(s)

تصميم و تركيب مركب عالجي محتمل من مشتقات كوينازولين-ليبويك أسيد لعالج مرض الزهايمر

Dissertant

al-Haddabi, Fatimah Muin Fadil

Thesis advisor

Abu al-Asal, Qays

University

Isra University

Faculty

Faculty of Pharmacy

University Country

Jordan

Degree

Master

Degree Date

2020

English Abstract

Alzheimer’s disease (AD) is one of most common neurodegenerative disorder and irreversible form of dementia in elderly people and the available treatment for this disease is only symptomatic and doesn’t delay the disease progression.

Alzheimer’s disease is multi-factorial disease involved several pathological hypothesis mainly cholinergic and oxidative stress hypothesis.

Quinazoline derivative moiety had been reported in many previous studies that had inhibition activity against acetylcholine esterase (AChE) the main enzyme in cholinergic hypothesis.

In this work we designed and synthesized a novel hybrid compound of quinazolinelipoic acid derivative (compound 5) which supposed to have dual activity to delay the progression of AD.

Compound 5 synthesis was started from N-methyl isatoic anhydride that react with aqueous ammonia to form compound 2 in 95% yield, compound 2 then reacted with cycloheptanone to form Spiro compound 3 in 94% yield.

Compound 3 then reduced to form compound 4 with 95% yield, compound 4 then coupled with lipoic acid using thionyl chloride, the reactions monitored with TLC and the final product characterized by GC-MS, H-NMR and C-NMR.

Compound 5 was synthesized in 25% yield and could biologically evaluated for its ability to inhibit AChE and its anti-oxidant activity as future work.

Main Topic

Pharmacology

No. of Pages

41

Table of Contents

Table of contents.

Abstract.

Abstract in Arabic.

Chapter One : Introduction.

Chapter Two : Previous studies.

Chapter Three : Materials and Methods.

Chapter Four : Experimental.

Chapter Five : Results and Discussion.

Chapter Six : Conclusions and recommendations.

References.

American Psychological Association (APA)

al-Haddabi, Fatimah Muin Fadil. (2020). Design and synthesis of a potential lead compound quinazoline-lipoic acid derivative for the treatment of Alzheimer’s disease. (Master's theses Theses and Dissertations Master). Isra University, Jordan
https://search.emarefa.net/detail/BIM-988934

Modern Language Association (MLA)

al-Haddabi, Fatimah Muin Fadil. Design and synthesis of a potential lead compound quinazoline-lipoic acid derivative for the treatment of Alzheimer’s disease. (Master's theses Theses and Dissertations Master). Isra University. (2020).
https://search.emarefa.net/detail/BIM-988934

American Medical Association (AMA)

al-Haddabi, Fatimah Muin Fadil. (2020). Design and synthesis of a potential lead compound quinazoline-lipoic acid derivative for the treatment of Alzheimer’s disease. (Master's theses Theses and Dissertations Master). Isra University, Jordan
https://search.emarefa.net/detail/BIM-988934

Language

English

Data Type

Arab Theses

Record ID

BIM-988934