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• W2016991826 abstract "The synthesis, molecular modeling, and pharmacological analysis of phenoxyalkylamino-4-phenylnicotinates (2-7), phenoxyalkoxybenzylidenemalononitriles (12, 13), pyridonepezils (14-18), and quinolinodonepezils (19-21) are described. Pyridonepezils 15-18 were found to be selective and moderately potent regarding the inhibition of hAChE, whereas quinolinodonepezils 19-21 were found to be poor inhibitors of hAChE. The most potent and selective hAChE inhibitor was ethyl 6-(4-(1-benzylpiperidin-4-yl)butylamino)-5-cyano-2-methyl-4-phenylnicotinate (18) [IC(50) (hAChE) = 0.25 ± 0.02 μM]. Pyridonepezils 15-18 and quinolinodonepezils 20-21 are more potent selective inhibitors of EeAChE than hAChE. The most potent and selective EeAChE inhibitor was ethyl 6-(2-(1-benzylpiperidin-4-yl)ethylamino)-5-cyano-2-methyl-4-phenylnicotinate (16) [IC(50) (EeAChE) = 0.0167 ± 0.0002 μM], which exhibits the same inhibitory potency as donepezil against hAChE. Compounds 2, 7, 13, 17, 18, 35, and 36 significantly prevented the decrease in cell viability caused by Aβ(1-42). All compounds were effective in preventing the enhancement of AChE activity induced by Aβ(1-42). Compounds 2-7 caused a significant reduction whereas pyridonepezils 17 and 18, and compound 16 also showed some activity. The pyrazolo[3,4-b]quinolines 36 and 38 also prevented the upregulation of AChE induced by Aβ(1-42). Compounds 2, 7, 12, 13, 17, 18, and 36 may act as antagonists of voltage sensitive calcium channels, since they significantly prevented the Ca(2+) influx evoked by KCl depolarization. Docking studies show that compounds 16 and 18 adopted different orientations and conformations inside the active-site gorges of hAChE and hBuChE. The structural and energetic features of the 16-AChE and 18-AChE complexes compared to the 16-BuChE and 18-BuChE complexes account for a higher affinity of the ligand toward AChE. The present data indicate that compounds 2, 7, 17, 18, and 36 may represent attractive multipotent molecules for the potential treatment of Alzheimer's disease." @default.
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• W2016991826 date "2013-02-04" @default.
• W2016991826 modified "2023-10-18" @default.
• W2016991826 title "Synthesis, Pharmacological Assessment, and Molecular Modeling of Acetylcholinesterase/Butyrylcholinesterase Inhibitors: Effect against Amyloid-β-Induced Neurotoxicity" @default.
• W2016991826 cites W1483073498 @default.
• W2016991826 cites W1616649812 @default.
• W2016991826 cites W1940331911 @default.
• W2016991826 cites W1963707072 @default.
• W2016991826 cites W1971048984 @default.
• W2016991826 cites W1976527379 @default.
• W2016991826 cites W1980314143 @default.
• W2016991826 cites W1982573845 @default.
• W2016991826 cites W1984960342 @default.
• W2016991826 cites W1993772503 @default.
• W2016991826 cites W1996894861 @default.
• W2016991826 cites W1997933391 @default.
• W2016991826 cites W2000075190 @default.
• W2016991826 cites W2001649679 @default.
• W2016991826 cites W2006102445 @default.
• W2016991826 cites W2006656242 @default.
• W2016991826 cites W2006734683 @default.
• W2016991826 cites W2009221410 @default.
• W2016991826 cites W2009277432 @default.
• W2016991826 cites W2009828191 @default.
• W2016991826 cites W2015859691 @default.
• W2016991826 cites W2017889639 @default.
• W2016991826 cites W2018342879 @default.
• W2016991826 cites W2021740591 @default.
• W2016991826 cites W2024921053 @default.
• W2016991826 cites W2025223727 @default.
• W2016991826 cites W2029901014 @default.
• W2016991826 cites W2033363151 @default.
• W2016991826 cites W2038212451 @default.
• W2016991826 cites W2041269990 @default.
• W2016991826 cites W2044075980 @default.
• W2016991826 cites W2046252479 @default.
• W2016991826 cites W2054910664 @default.
• W2016991826 cites W2059937283 @default.
• W2016991826 cites W2060241841 @default.
• W2016991826 cites W2064086864 @default.
• W2016991826 cites W2064097612 @default.
• W2016991826 cites W2064340111 @default.
• W2016991826 cites W2064604574 @default.
• W2016991826 cites W2078179976 @default.
• W2016991826 cites W2081912151 @default.
• W2016991826 cites W2084107396 @default.
• W2016991826 cites W2086458951 @default.
• W2016991826 cites W2087903983 @default.
• W2016991826 cites W2089688642 @default.
• W2016991826 cites W2092677781 @default.
• W2016991826 cites W2093658660 @default.
• W2016991826 cites W2100969363 @default.
• W2016991826 cites W2110831253 @default.
• W2016991826 cites W2112642170 @default.
• W2016991826 cites W2118200955 @default.
• W2016991826 cites W2124362440 @default.
• W2016991826 cites W2135134122 @default.
• W2016991826 cites W2137777161 @default.
• W2016991826 cites W2142093490 @default.
• W2016991826 cites W2145810295 @default.
• W2016991826 cites W2146158590 @default.
• W2016991826 cites W2152301430 @default.
• W2016991826 cites W2159866533 @default.
• W2016991826 cites W2161127424 @default.
• W2016991826 cites W2162166182 @default.
• W2016991826 cites W2289453788 @default.
• W2016991826 cites W2949155749 @default.
• W2016991826 cites W2950508524 @default.
• W2016991826 cites W4242215325 @default.
• W2016991826 doi "https://doi.org/10.1021/cn300178k" @default.
• W2016991826 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3629749" @default.
• W2016991826 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/23379636" @default.
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