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
Anu Rani
1
,
Amandeep Singh
1
,
Jashanpreet Kaur
2
,
Gurjit Singh
2
,
Abhishek Jain
2
,
Njabulo Joyfull Gumede
3
,
Prishani Kisten
4
,
Parvesh Singh
4
,
Sumanjit
1
,
Vipan Kumar
1
3
Department of Chemistry, Mangosuthu University of Technology, P.O. Box 12363, Jacobs 4026, South Africa.
|
Publication type: Journal Article
Publication date: 2021-09-01
scimago Q1
wos Q1
SJR: 0.786
CiteScore: 8.3
Impact factor: 4.7
ISSN: 00452068, 10902120
PubMed ID:
34120027
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Abstract
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.
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Rani A. et al. 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 // Bioorganic Chemistry. 2021. Vol. 114. p. 105053.
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Rani A., Singh A., Kaur J., Singh G., Jain A., Gumede N. J., Kisten P., Singh P., Sumanjit, Kumar V. 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 // Bioorganic Chemistry. 2021. Vol. 114. p. 105053.
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TY - JOUR
DO - 10.1016/j.bioorg.2021.105053
UR - https://doi.org/10.1016/j.bioorg.2021.105053
TI - 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
T2 - Bioorganic Chemistry
AU - Rani, Anu
AU - Singh, Amandeep
AU - Kaur, Jashanpreet
AU - Singh, Gurjit
AU - Jain, Abhishek
AU - Gumede, Njabulo Joyfull
AU - Kisten, Prishani
AU - Singh, Parvesh
AU - Sumanjit
AU - Kumar, Vipan
PY - 2021
DA - 2021/09/01
PB - Elsevier
SP - 105053
VL - 114
PMID - 34120027
SN - 0045-2068
SN - 1090-2120
ER -
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BibTex (up to 50 authors)
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@article{2021_Rani,
author = {Anu Rani and Amandeep Singh and Jashanpreet Kaur and Gurjit Singh and Abhishek Jain and Njabulo Joyfull Gumede and Prishani Kisten and Parvesh Singh and Sumanjit and Vipan Kumar},
title = {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},
journal = {Bioorganic Chemistry},
year = {2021},
volume = {114},
publisher = {Elsevier},
month = {sep},
url = {https://doi.org/10.1016/j.bioorg.2021.105053},
pages = {105053},
doi = {10.1016/j.bioorg.2021.105053}
}