Design,Synthesis, Biological Evaluation,and Docking Study of Acetylcholinesterase Inhibitors: New Acridone‐1,2,4‐oxadiazole‐1,2,3‐triazole Hybrids |
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| Authors: | Maryam Mohammadi‐Khanaposhtani Mohammad Mahdavi Mina Saeedi Reyhaneh Sabourian Maliheh Safavi Mahnaz Khanavi Alireza Foroumadi Abbas Shafiee Tahmineh Akbarzadeh |
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| Institution: | 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran;2. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran;3. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran;4. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran;5. Department of Biotechnology, Iranian Research Organization for Science and Technology, Tehran, Iran;6. Department of Pharmacognosy, Tehran University of Medical Sciences, Tehran, Iran |
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| Abstract: | In this study, novel acridone‐1,2,4‐oxadiazole‐1,2,3‐triazole hybrids were designed, synthesized, and evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activity. Among various synthesized compounds, 10‐((1‐((3‐(4‐methoxyphenyl)‐1,2,4‐oxadiazol‐5‐yl)methyl)‐1H‐1,2,3‐triazol‐4‐yl)methyl)acridin‐9(10H)‐one 10b showed the most potent anti‐acetylcholinesterase activity (IC50 = 11.55 μm ) being as potent as rivastigmine. Also docking outcomes were in good agreement with in vitro results confirming the dual binding inhibitory activity of compound 10b . |
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| Keywords: | acetylcholinesterase acridone‐1 2 4‐oxadiazole‐1 2 3‐triazole Alzheimer's disease docking study |
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