Sadashiva, C. T. and Narendra Sharath Chandra, J. N. and Ponnappa, K. C. and Veerabasappa Gowda, T. and Rangappa, K. S. (2006) Synthesis and efficacy of 1-bis(4-fluorophenyl)-methylpiperazine derivatives for acetylcholinesterase inhibition, as a stimulant of central cholinergic neurotransmission in Alzheimer’s disease. Bioorganic & Medicinal Chemistry Letters, 16 (15). 3932 - 3936. ISSN 1464-3405
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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)-methylpiperazine derivatives were synthesized under mild conditions using different aryl/alkyl halides and heterocyclic alkyl halides with 1-bis(4-fluorophenyl)-methylpiperazine 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.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Piperazine, AchE, Rodent memory evaluator, Alzheimer’s disease |
| Subjects: | C Chemical Science > Chemistry |
| Divisions: | Department of > Chemistry |
| Depositing User: | LA manjunath user |
| Date Deposited: | 17 Aug 2019 09:32 |
| Last Modified: | 07 Jul 2022 07:39 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/6664 |
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