Literature DB >> 19717214

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

C T Sadashiva1, J N Narendra Sharath Chandra, C V Kavitha, A Thimmegowda, M N Subhash, Kanchugarakoppal S Rangappa.   

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.

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Year:  2009        PMID: 19717214     DOI: 10.1016/j.ejmech.2009.07.026

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  5 in total

Review 1.  Alzheimer's disease and age-related memory decline (preclinical).

Authors:  Alvin V Terry; Patrick M Callahan; Brandon Hall; Scott J Webster
Journal:  Pharmacol Biochem Behav       Date:  2011-02-24       Impact factor: 3.533

2.  Multitarget Effect of 2-(4-(Methylthio)phenyl)-3-(3-(piperidin-1-yl)propyl)thiazolidin-4-one in a Scopolamine-Induced Amnesic Rat Model.

Authors:  Daniel Schuch da Silva; Mayara Sandrielly Pereira Soares; Fernanda Cardoso Teixeira; Júlia Eisenhardt de Mello; Anita Avila de Souza; Karina Pereira Luduvico; Cinthia Melazzo de Andrade; Roselia Maria Spanevello; Wilson Cunico
Journal:  Neurochem Res       Date:  2021-03-23       Impact factor: 3.996

3.  Synthesis, In Silico and Pharmacological Evaluation of New Thiazolidine-4-Carboxylic Acid Derivatives Against Ethanol-Induced Neurodegeneration and Memory Impairment.

Authors:  Shagufta Naz; Lina Tariq Al Kury; Humaira Nadeem; Fawad Ali Shah; Aman Ullah; Rehan Zafar Paracha; Muhammad Imran; Shupeng Li
Journal:  J Inflamm Res       Date:  2022-06-25

4.  Improvement of autophagic flux mediates the protection of hydrogen sulfide against arecoline-elicited neurotoxicity in PC12 cells.

Authors:  Sheng-Lan Gao; Yi-Yun Tang; Jia-Mei Jiang; Wei Zou; Ping Zhang; Xiao-Qing Tang
Journal:  Cell Cycle       Date:  2022-03-22       Impact factor: 5.173

5.  Arecoline Induces Neurotoxicity to PC12 Cells: Involvement in ER Stress and Disturbance of Endogenous H2S Generation.

Authors:  Jia-Mei Jiang; Li Wang; Hong-Feng Gu; Keng Wu; Fan Xiao; Ying Chen; Run-Min Guo; Xiao-Qing Tang
Journal:  Neurochem Res       Date:  2016-06-02       Impact factor: 3.996

  5 in total

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