2013
DOI: 10.1021/cn300178k
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Synthesis, Pharmacological Assessment, and Molecular Modeling of Acetylcholinesterase/Butyrylcholinesterase Inhibitors: Effect against Amyloid-β-Induced Neurotoxicity

Abstract: 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)butylam… Show more

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Cited by 53 publications
(36 citation statements)
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“…[ [4][5][6] Two cholinesterases, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), are responsible for hydrolysis of the neurotransmitter ACh in the brain. Recent evidence has highlighted a non-classical role for cholinergic enzymes, which may be important for the development of more effective drugs for AD.…”
Section: Introductionmentioning
confidence: 99%
“…[ [4][5][6] Two cholinesterases, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), are responsible for hydrolysis of the neurotransmitter ACh in the brain. Recent evidence has highlighted a non-classical role for cholinergic enzymes, which may be important for the development of more effective drugs for AD.…”
Section: Introductionmentioning
confidence: 99%
“…Diverse pyrazole derivatives (Compounds 76 – 81 ; Silva et al, ; Silva, Samadi, Chioua, Carreiras, & Marco‐Contelles, ) and (phenoxyalkoxybenzylidenemalononitriles (Compounds 81 and 82 ; Silva et al, ) were previously synthesized and their AChE inhibitory activities reported. Here we describe their inhibitory activities in rat mitochondria (rMAO A and rMAO B; Table S2).…”
Section: Resultsmentioning
confidence: 99%
“…Neurological disorders, such as Alzheimer's disease, senile dementia, ataxia and myasthenia gravis, are related to AChE, and AChE inhibitors are meant to inhibit the AChE enzyme in order to enhance muscle contraction and strengthen the cholinergic neurotransmission [27]. White zones on a violet plate background represented AChE inhibiting compounds (Figure 3, #4 A-C).…”
Section: Detection Of Ache Inhibitory Compoundsmentioning
confidence: 99%