Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 15, Pages 3932-3936Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.05.030
Keywords
piperazine; AchE; rodent memory evaluator; Alzheimer's disease
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The cholinergic hypothesis of Alzheimer's disease (AD) has spurred the development of numerous structural classes of compounds with different pharmacological profile aimed at increasing central cholinergic neurotransmission. Thus proving a symptomatic treatment for this disease are cholinomimetics with the pharmacological profile of acetyl cholinesterase (AchE) inhibitors. The novel bioactive 1-[bis(4-fluorophenyl)-methyl]piperazine derivatives were synthesized under mild conditions using different aryl/ alkyl halides and heterocyclic alkyl halides with 1-[bis(4-fluorophenyl)-methyl]piperazine in the presence of powdered potassium carbonate in N,N-dimethylformamide. All the synthesized compounds were characterized by spectroscopic techniques, elemental analysis and were screened for their efficacy as AchE inhibitor. Some derivatives in this class showed good inhibition against AchE as compared to neostigmine as standard. (c) 2006 Elsevier Ltd. All rights reserved.
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