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Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-Oxadiazole-1,2,3-Triazole Hybrids Publisher Pubmed



Mohammadikhanaposhtani M1 ; Mahdavi M2 ; Saeedi M3 ; Sabourian R4 ; Safavi M5 ; Khanavi M6 ; Foroumadi A2 ; Shafiee A2 ; Akbarzadeh T1, 4
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 14176, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran
  3. 3. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 14176, Iran
  4. 4. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran
  5. 5. Department of Biotechnology, Iranian Research Organization for Science and Technology, Tehran, 14176, Iran
  6. 6. Department of Pharmacognosy, Tehran University of Medical Sciences, Tehran, 14176, Iran

Source: Chemical Biology and Drug Design Published:2015


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. A novel series of acridone-1,2,4-oxadiazole-1,2,3-triazole hybrids were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. © 2015 John Wiley & Sons A/S.
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