الإشراف على رسائل الماجستير

  Rational design,synthesis and enzymatic evaluation of spiroquinazoline dervatives as novel inhibitors of acetylcholinesterase
تاريخ مجلس الدراسات العليا
2021-06-23
اسم الطالب
شهد وجيه ياسين ياسين
ملخص الرسالة
Alzheimer's disease has been one of the most infuriating disease for elderly people round the world. It is characterized by memory loss and cognitive impairment, mostly because of injury of cholinergic neurons in the hippocampus and forebrain beside dropping of the amount of acetylcholine (ACh), which is one of the major causes of the oxidative stress by RNS and ROS in many regions in the brain. Present treatments which are available for this neuro degenerative disease is chiefly symptomatic, hence they are not dealing the disease progression. Quinazoline compounds are promising lead for many researchers due to their capability to inhibit AChE and their ability as free radical species that serve as scavenging agents. In this work , we report the synthesis of several quinazoline derivatives 3-5 in a good yield. The structure of synthesized compounds was confirmed with GC-MS, 1H and 13C-NMR. Acetylcholine esterase inhibition was studied utilizing Ellman's method, and IC50 values were determined showing a potent inhibitory activity of our synthesized compounds. In vitro, compounds 3-5 against AChE enzyme demonstrated a potent inhibitory activity and could be potential lead compounds for further development.