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Synthesis and biological evaluation of some novel coumarin derivatives of expected cholinesterase inhibitory activity /

Mennat Allah Mohammed Mahmoud Elsawah

Synthesis and biological evaluation of some novel coumarin derivatives of expected cholinesterase inhibitory activity / التشييد و التقييم الحيوى لبعض مشتقات الكومارين الجديدة المتوقع لها نشاط مثبط لإنزيم الكولين إستريز Mennat Allah Mohammed Mahmoud Elsawah ; Supervised Kamilia Mahmoud Amin , Yassin Mohammed Nissan , Walaa Ramadan Mahmoud - Cairo : Mennat Allah Mohammed Mahmoud Elsawah , 2018 - 161 P. ; 25cm

Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

Coumarin is an interesting bioactive scaffold eliciting a wide range of biological activities including anticancer, antibacterial, anti-inflammatory, antihypertensive and anticonvulsant activity. Herein, we highlighted on the acetylcholinesterase inhibitory activity of the coumarin nucleus notably 6-aminocoumarin derivatives which were reported to possess acetylcholinesterase inhibitory activity and many of them are in clinical trials. In this work, six series of 6-aminocoumarin-based compounds were synthesized. The target compounds featured a variety of bioactive chemical fragments of CNS action. Acetylcholinesterase inhibitory activity study was performed for all synthesized compounds. Furthermore, in silico studies were performed on the synthesized compounds which included molecular docking study at the active site of AChE enzyme as well as prediction of their pharmacokinetic parameters



Acetylcholinesterase Alzehimers Coumarin