title: Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.
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.
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 14176, Iran.
authors.forename: Maryam
authors.initials: M
authors.lastname: Mohammadi-Khanaposhtani
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Mahdavi
authors.affiliation: Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 14176, Iran.|Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran.
authors.forename: Mina
authors.initials: M
authors.lastname: Saeedi
authors.affiliation: Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran.
authors.forename: Reyhaneh
authors.initials: R
authors.lastname: Sabourian
authors.affiliation: Department of Biotechnology, Iranian Research Organization for Science and Technology, Tehran, 14176, Iran.
authors.forename: Maliheh
authors.initials: M
authors.lastname: Safavi
authors.affiliation: Department of Pharmacognosy, Tehran University of Medical Sciences, Tehran, 14176, Iran.
authors.forename: Mahnaz
authors.initials: M
authors.lastname: Khanavi
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran.
authors.forename: Alireza
authors.initials: A
authors.lastname: Foroumadi
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran.
authors.forename: Abbas
authors.initials: A
authors.lastname: Shafiee
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 14176, Iran.|Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran.
authors.forename: Tahmineh
authors.initials: T
authors.lastname: Akbarzadeh
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry; D054831:Acridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020134:Catalytic Domain; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D016166:Free Radical Scavengers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006860:Hydrogen Bonding; D062105:Molecular Docking Simulation; D013329:Structure-Activity Relationship
chemical_list: D054831:Acridones; D000975:Antioxidants; D002800:Cholinesterase Inhibitors; D016166:Free Radical Scavengers; D000110:Acetylcholinesterase
keywords: Alzheimer's disease; acetylcholinesterase; acridone-1,2,4-oxadiazole-1,2,3-triazole; docking study