1H-1,2,3-triazole grafted tacrine-chalcone conjugates as potential cholinesterase inhibitors with the evaluation of their behavioral tests and oxidative stress in mice brain cells
| Autor: | Rajbir Bhatti, Prishani Kisten, Sumanjit, Njabulo J. Gumede, Vipan Kumar, Jashanpreet Kaur, Anu Rani, Amandeep Singh, Parvesh Singh, Gurjit Singh |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Chalcone
Anxiety Pharmacology medicine.disease_cause 01 natural sciences Biochemistry Lipid peroxidation Mice Structure-Activity Relationship chemistry.chemical_compound Chalcones Drug Discovery medicine TBARS Animals Molecular Biology Butyrylcholinesterase Cholinesterase Dose-Response Relationship Drug Molecular Structure biology Depression 010405 organic chemistry Chemistry Organic Chemistry Brain Glutathione Triazoles Rats 0104 chemical sciences Molecular Docking Simulation Oxidative Stress 010404 medicinal & biomolecular chemistry Tacrine Acetylcholinesterase biology.protein Cholinesterase Inhibitors Oxidative stress medicine.drug |
| Zdroj: | Bioorganic Chemistry. 114:105053 |
| ISSN: | 0045-2068 |
| DOI: | 10.1016/j.bioorg.2021.105053 |
| Popis: | The present paper explicates the synthesis of 1H-1,2,3-triazole tethered tacrine-chalcone conjugates and evaluation of their AChE and BuChE inhibitory activity. In-vitroAChE inhibition assay revealed three compounds, 9h, 9i, and 11f, being more potent than the standard drug tacrine and further evaluated against butyrylcholinesterase. The present study was extended to investigate the anti-amnestic effect of promising compoundson scopolamine-induced behavioral and neurochemical changes in mice. Inclined plane model and Elevated plus-maze model were performed to assess general limb motor activity and anxiety-like behavior, respectively, in mice pre-treated with scopolamine. Oxidative stress parameters reduced glutathione contents (GSH) and lipid peroxidation products (TBARS) in the brain homogenates as estimated using ex-vivo studies. Furthermore, molecular docking studies were performed for the potent compounds to decipher the mechanism of observed activities. |
| Databáze: | OpenAIRE |
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