الإشراف على رسائل الماجستير
Synthesis the characterization of quinazoline-cinnamic acid hybrid as alzhemer drug candidate
تاريخ مجلس الدراسات العليا
2020-06-11
اسم الطالب
ضحى محسن عبدالحسين الظالمي
ملخص الرسالة
Alzheimer's disease (AD) has been one of the most important cause of death for elderly people around the world. It's characterized by cognitive impairment and memory loss, mainly because of damage of cholinergic neurons in the fore-brain and hippocampus and reducing amount of Acetylcholine as well, the second main cause is the oxidative stress by reactive oxygen species (ROS) and reactive nitrogen species (RNS) in many brain region. Current treatment available for this neurodegenerative disease was mainly symptomatic and they were not affected on disease progression. Quinazoline moiety as promising structure in many research has the ability to inhibit acetylcholine esterase (AChE) enzyme and the ability of free radical scavenging. We decided to design and synthesize a novel hybrid compound 5 (quinazoline- cinnamic acid) that supposed to have a dual biological activity to delay the progression of AD. Synthesis of final hybrid compound was done through several reaction starting from N-methylisatoic anhydride which reacted with aqueous ammonia to form compound 2 with 90% yield. Second step involved synthesis of spiro compound (3) with 90% yeild by reacted compound 2 with cyclopentanone. Compound 4 was synthesized with 94% yield by reduction of compound 3 using LiAlH4 and compound 5 was synthesized in 46% of yield. All reactions involved was monitored using TLC and GC-MS and characterized their final product by H-NMR and C-NMR. In future, the hybrid compound 5 as potential drug candidate for AD could be biologically evaluated for its ability to inhibit AChE enzyme and its antioxidant activity.