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العنوان
Synthesis of Heterocyclic Analogs As Agents for Potential Treatment of Alzheimer’s Disease
الناشر
Alexandria University. faculty of Pharmacy. Department of Pharmaceutical Chemistry,
المؤلف
Ragab, Hanan Mohamed Ahmed
هيئة الاعداد
باحث / حنان محمد احمد رجب
مشرف / احمد محسن محمد
مشرف / فوزية احمد عاشور
مناقش / علاء احمد
تاريخ النشر
2007 .
عدد الصفحات
160p.
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
الصيدلة ، علم السموم والصيدلانيات
تاريخ الإجازة
1/1/2007
مكان الإجازة
جامعة الاسكندريه - كلية الصيدلة - Pharmaceutical Chemistry
الفهرس
Only 14 pages are availabe for public view

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from 196

Abstract

Alzheimer’s disease (AD) is known to cause a major health problem affecting a large population worldwide.
Researchers, working to find out a remedy for AD, have synthesized a large number of compounds targeting the potentiation of cholinergic activity in the brain. Among these compounds, anti-cholinesterase inhibitors have been the most extensively studied group.
Due to the adverse effects associated with the use of acetyl cholinesterase inhibitors, researches have now been directed to cholinergic agonists. Considerable interest in CNS nicotinic receptors developed when several laboratories almost simultaneously reported drastic (>50%) losses in cerebral cortex high affinity nicotinic receptors in Alzheimer’s disease, while changes in muscarinic receptors were relatively quite small.
These facts initiated the synthesis of three series of compounds as potential 7 nicotinic ligands for treatment of Alzheimer’s disease.
The studies, constituting the text of this thesis, are presented in various chapters as follows:
Introduction:
It comprises a review of the literature showing the various approaches for treatment of Alzheimer’s disease and the drugs involved in each respect.
Tacrine, Donepezil, Rivastigmine and Galanthamine were presesented as important cholinesterase inhibitors with high efficacy in treatment of Alzheimer’s disease.
Arecoline and Xanomeline were presented as representative examples of the muscarinic agonists
Finally, nicotinic agonists were presented as an important future approach for treatment of AD. Affinity for 7 nAChR led to development of some nicotinic ligands as F3, Anabaseine, GTS-21, AR-R17779 and their derivatives.
Structure-activity relationship of several examples of these classes of compounds has been presented to deduce the functional groups responsible for respective biological activity.
Aim of the work:
This part deals with the chemical and biological bases on which the target compounds were designed.