تاريخ مجلس الدراسات العليا

2020-07-01

اسم الطالب

فاطمة معين فاضل الهدابي

ملخص الرسالة

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 quinazoline-lipoic 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.