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For this purpose, a novel series of hydrazone derivatives containing imidazolidine ring aimed against Alzheimer's disease (AD), have been designed and synthesized. The acetylcholinesterase (AChE) enzyme inhibitory activity of these compounds was investigated. The structures of the compounds were determined by IR, <jats:sup>1<\/jats:sup>H and <jats:sup>13<\/jats:sup>C\u2010NMR and mass spectroscopic methods. Inhibition studies on the cholinesterase (ChE) enzymes and \u03b2\u2010amyloid plaque inhibition test of the compounds were performed. Based on the experimental results, compound <jats:bold>3j<\/jats:bold> bearing dimethoxy substituent on the aromatic ring like donepezil exhibited the most AChE inhibitory activity with the IC<jats:sub>50<\/jats:sub> values of 0.023\u00b10.001\u2005\u03bcM. Owing to obtained biological activity and molecular docking study results, it is thought that the most active compound <jats:bold>3j<\/jats:bold> may play a role in both symptomatic and palliative treatment of AD.<\/jats:p>","DOI":"10.1002\/cbdv.202200265","type":"journal-article","created":{"date-parts":[[2022,6,28]],"date-time":"2022-06-28T06:03:35Z","timestamp":1656396215000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["<i>N<\/i>\u2010Substituted Arylidene\u20103\u2010(Methylsulfonyl)\u20102\u2010Oxoimidazolidine\u20101\u2010Carbohydrazide as Cholinesterase Inhibitors: Design, Synthesis, and Molecular Docking Study"],"prefix":"10.1002","volume":"19","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-4569-008X","authenticated-orcid":false,"given":"Fatih","family":"Tok","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Chemistry Faculty of Pharmacy Marmara University  34854 Istanbul Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Beg\u00fcm Nurpelin","family":"Sa\u011fl\u0131k","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Faculty of Pharmacy Anadolu University  26470 Eski\u015fehir Turkey"},{"name":"Doping and Narcotic Compounds Analysis Laboratory Faculty of Pharmacy Anadolu University  26470 Eski\u015fehir Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yusuf","family":"\u00d6zkay","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Faculty of Pharmacy Anadolu University  26470 Eski\u015fehir Turkey"},{"name":"Doping and Narcotic Compounds Analysis Laboratory Faculty of Pharmacy Anadolu University  26470 Eski\u015fehir Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zafer As\u0131m","family":"Kaplanc\u0131kl\u0131","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Faculty of Pharmacy Anadolu University  26470 Eski\u015fehir Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bedia","family":"Ko\u00e7yi\u011fit\u2010Kaymak\u00e7\u0131o\u011flu","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Faculty of Pharmacy Marmara University  34854 Istanbul Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2022,7,7]]},"reference":[{"key":"e_1_2_7_1_1","doi-asserted-by":"publisher","DOI":"10.3233\/JAD-180766"},{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1002\/JLB.MR0818-319R"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules25245789"},{"key":"e_1_2_7_4_1","unstructured":"M. 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