Synthesis and efficacy of 1-[bis(4-fluorophenyl)-methyl]piperazine derivatives for acetylcholinesterase inhibition, as a stimulant of central cholinergic neurotransmission in Alzheimer's disease.

Abstract

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.

• Authors: C T Sadashiva, J N Narendra Sharath Chandra, K C Ponnappa, T Veerabasappa Gowda, Kanchugarakoppal S Rangappa
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 16 Issue 15 Pg. 3932-6 (Aug 01 2006) ISSN: 0960-894X [Print] England
• PMID: 16735118 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Cholinesterase Inhibitors
• Piperazines
• Acetylcholinesterase

Topics

• Acetylcholinesterase (drug effects)
• Alzheimer Disease (enzymology, physiopathology)
• Cholinesterase Inhibitors (chemical synthesis, chemistry, pharmacology)
• Humans
• Piperazines (chemical synthesis, chemistry, pharmacology)
• Structure-Activity Relationship
• Synaptic Transmission (drug effects)