Synthesis and pharmacological evaluation of novel N-alkyl/aryl substituted thiazolidinone arecoline analogues as muscarinic receptor 1 agonist in Alzheimer's dementia models

Sadashiva, C. T. and Narendra Sharath Chandra, J. N. and Kavitha, C. V. and Thimmegowda, A. and Subhash, M. N. and Rangappa, K. S. (2009) Synthesis and pharmacological evaluation of novel N-alkyl/aryl substituted thiazolidinone arecoline analogues as muscarinic receptor 1 agonist in Alzheimer's dementia models. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 44 (12). pp. 4848-4854. ISSN 1768-3254

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Official URL: http://doi.org/10.1016/j.ejmech.2009.07.026

Abstract

Earlier we have reported the effect of arecoline thiazolidinone and morpholino arecoline analogues as muscarinic receptor 1 agonist in Alzheimer's dementia models. To elucidate further our SAR study on the chemistry and muscarinic receptor binding efficacy, a series of novel N-alkyl/aryl substituted thiazolidinone arecoline analogues 6(a-m) were designed and synthesized from 3-pyridine carboxaldehyde by reacting with different amines in the presence of gamma-ferrite as catalyst and subjected to in vitro muscarinic receptor binding studies using male Wistar rat brain membrane homogenate and extended to in vivo pharmacological evaluation of memory and learning in male Wistar rats. Derivative 6j having diphenylamine moiety attached to nitrogen of thiazolidinone showed significant affinity for the M1 receptor binding. (C) 2009 Elsevier Masson SAS. All rights reserved.

Item Type: Article
Uncontrolled Keywords: M1 receptor binding; Alzheimer's disease; Arecoline derivatives; Thiazolidinones
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Users 19 not found.
Date Deposited: 13 Aug 2019 05:17
Last Modified: 13 Aug 2019 05:17
URI: http://eprints.uni-mysore.ac.in/id/eprint/6301

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