{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Wan LX"],"funding":["Ministry of Education of the People&apos;s Republic of China","National Natural Science Foundation of China","Research Foundation for Administration of traditional Chinese Medicine of Sichuan Province"],"pagination":["23347-23354"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8444293"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["6(36)"],"pubmed_abstract":["Palladium/BuAd<sub>2</sub>P efficiently catalyzed the direct α-arylation of ketone in the anti-Alzheimer's disease drug donepezil, leading to 15 aryldonepezil analogues exhibiting high selective inhibition of acetylcholinesterase (AChE). The cell-based assays revealed that the 3-methylpridinyl analogue (<b>12</b>) shows significantly lower toxicity compared to donepezil and remarkable neuroprotective activity against H<sub>2</sub>O<sub>2</sub>-induced damage in SH-SY5Y cells. Docking results of compound <b>12</b> also interpreted the possible mechanism of the selective inhibition between AChE and butyrylcholinesterase (BuChE)."],"journal":["ACS omega"],"pubmed_title":["Pd-Catalyzed Direct Modification of an Anti-Alzheimer's Disease Drug: Synthesis and Biological Evaluation of α-Aryl Donepezil Analogues."],"pmcid":["PMC8444293"],"funding_grant_id":["82003634","YGJH2020-LY06","2020HJZX002","31870329","81773605"],"pubmed_authors":["Li X","He ZX","Wan LX","Zhou XL","Miao SX","Gao F"],"additional_accession":[]},"is_claimable":false,"name":"Pd-Catalyzed Direct Modification of an Anti-Alzheimer's Disease Drug: Synthesis and Biological Evaluation of α-Aryl Donepezil Analogues.","description":"Palladium/BuAd<sub>2</sub>P efficiently catalyzed the direct α-arylation of ketone in the anti-Alzheimer's disease drug donepezil, leading to 15 aryldonepezil analogues exhibiting high selective inhibition of acetylcholinesterase (AChE). The cell-based assays revealed that the 3-methylpridinyl analogue (<b>12</b>) shows significantly lower toxicity compared to donepezil and remarkable neuroprotective activity against H<sub>2</sub>O<sub>2</sub>-induced damage in SH-SY5Y cells. Docking results of compound <b>12</b> also interpreted the possible mechanism of the selective inhibition between AChE and butyrylcholinesterase (BuChE).","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Sep","modification":"2024-02-14T20:12:04.259Z","creation":"2022-02-11T11:08:15.169Z"},"accession":"S-EPMC8444293","cross_references":{"pubmed":["34549134"],"doi":["10.1021/acsomega.1c03103"]}}