الإشراف على رسائل الماجستير

  Synthesis of novel tetrahydro quinazoline-antioxidant hybrids as potential drugs against Alzheimer s disease.
نوع المشرف
مشرف رئيسي
تاريخ الاشراف على الرسالة من
الى
2022
اسم الطالب
Mohammed Khalaf Rashid
ملخص الرسالة
Alzheimer`s disease (AD) is the most significant public source of mortality among the older people across the world. Alzheimer's disease it`s 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 Alzheimer's disease, 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 LCMS, 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 anticholineresterase activity showed significant dose-dependent inhibition of the enzyme by compound 5 (IC50 = 11.89λg / ml, p <0.05) comparable to the galantamine standard (IC50 = 9.570λg / ml). The compounds we have created have significant inhibitory activity and may be suitable lead compounds for development.