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Quercetin-1,2,3-Triazole Hybrids as Multifunctional Anti-Alzheimer's Agents. | LitMetric

Quercetin-1,2,3-Triazole Hybrids as Multifunctional Anti-Alzheimer's Agents.

Molecules

Department of Chemistry and Biochemistry, School of Sciences and Technologies, University of Évora, Rua Romão Ramalho 59, 7000-671 Évora, Portugal.

Published: November 2023

AI Article Synopsis

Article Abstract

The number of patients with Alzheimer's disease (AD) continues to rise and, despite the efforts of researchers, there are still no effective treatments for this multifaceted disease. The main objective of this work was the search for multifunctional and more effective anti-Alzheimer agents. Herein, we report the evaluation of a library of quercetin-1,2,3-triazole hybrids () in antioxidant, hydrogen peroxide-induced oxidative stress protection, and cholinesterases (AChE and BuChE) inhibitory activities. Hybrids and showed potent in vitro inhibitory activity on BuChE (IC values between 11.2 and 65.7 μM). Hybrid , the best inhibitor, was stronger than galantamine, displaying an IC value of 11.2 μM for BuChE, and is also a competitive inhibitor. Moreover, toxicity evaluation for the most promising hybrids was performed using the toxicity assay, showing low toxicity. Hybrids , and did not affect viability at 12.5 μM and also displayed a protective effect against oxidative stress induced by hydrogen peroxide in cell damage in MCF-7 cells. Hybrids , and act as multifunctional ligands in AD pathologies.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10673615PMC
http://dx.doi.org/10.3390/molecules28227495DOI Listing

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