Synthesis and Docking Studies of a Novel Tetrahydroquinazoline Derivative as Promising Scaffold for Acetylcholine Esterase Inhibition
Alsuhaimat, R., Abualassal, Q., abudyah, Z., Ebada, S., Albohy, A. (2020). Synthesis and Docking Studies of a Novel Tetrahydroquinazoline Derivative as Promising Scaffold for Acetylcholine Esterase Inhibition. EKB Journal Management System, 63(12), 4797-4804. doi: 10.21608/ejchem.2020.27985.2588
Rawan A. Alsuhaimat; Qais Abualassal; zead abudyah; Sherif S. Ebada; Amgad Albohy. "Synthesis and Docking Studies of a Novel Tetrahydroquinazoline Derivative as Promising Scaffold for Acetylcholine Esterase Inhibition". EKB Journal Management System, 63, 12, 2020, 4797-4804. doi: 10.21608/ejchem.2020.27985.2588
Alsuhaimat, R., Abualassal, Q., abudyah, Z., Ebada, S., Albohy, A. (2020). 'Synthesis and Docking Studies of a Novel Tetrahydroquinazoline Derivative as Promising Scaffold for Acetylcholine Esterase Inhibition', EKB Journal Management System, 63(12), pp. 4797-4804. doi: 10.21608/ejchem.2020.27985.2588
Alsuhaimat, R., Abualassal, Q., abudyah, Z., Ebada, S., Albohy, A. Synthesis and Docking Studies of a Novel Tetrahydroquinazoline Derivative as Promising Scaffold for Acetylcholine Esterase Inhibition. EKB Journal Management System, 2020; 63(12): 4797-4804. doi: 10.21608/ejchem.2020.27985.2588

Synthesis and Docking Studies of a Novel Tetrahydroquinazoline Derivative as Promising Scaffold for Acetylcholine Esterase Inhibition

Egyptian Journal of Chemistry
Article 13, Volume 63, Issue 12, December 2020, Page 4797-4804  XML PDF (1.37 MB)
Document Type: Original Article
DOI: 10.21608/ejchem.2020.27985.2588
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Authors
Rawan A. Alsuhaimat1; Qais Abualassal2; zead abudyah3; Sherif S. Ebada4; Amgad Albohy email orcid 5
1Faculty of Pharmacy, Mu’tah University, Al-Karak, 61166, Amman, Jordan
2Department of Applied Pharmaceutical Sciences, Faculty of Pharmacy, Isra University, Amman, Jordan
3Faculty of pharmacy / AL-isra university Amman / Jordan
4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mu’tah University, Al-Karak, Jordan. and Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University, Cairo, Egypt
5Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt (BUE), Egypt
Abstract
Alzheimer’s disease (AD) is one of the most prevalent neurodegenerative disorder. While pathological hallmarks of this disorder are known, the exact cause of AD remains unclear. Quinazoline was found to be a promising scaffold for the design and development of Acetylcholinesterase (AChE) inhibitors. In this study we report the synthesis of 1'-methyl-3', 4'-dihydro1'H-spiro[cyclopentane-1, 2'-quinazoline] (4) in 73.3% yield. The structure of compound 4 was confirmed with GC-MS, 1H and 13C-NMR. Acetylcholine esterase inhibition was studied virtually with docking into AChE active site and suggests potential use of 4 as a promising scaffold for acetylcholine esterase inhibitor design which might be useful for Alzheimer’s disease.
Keywords
Acetylcholine esterase inhibitor; Alzheimer disease; Quinazoline derivatives; Spiro compounds; Molecular Docking
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