ArticleAntioxidants (Basel, Switzerland)2021
Bisavenathramide Analogues as Nrf2 Inductors and Neuroprotectors in In Vitro Models of Oxidative Stress and Hyperphosphorylation.
Article in Antioxidants (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 21 citations in OpenAlex.
- Discovery of 15-deoxynaphthomycins activating the antioxidant NRF2-ARE pathway from Streptomyces sp. N50 via genome mining, global regulator introduction, and molecular networking.Microbial cell factories · 2025Article
- Fluorimetric Detection of Insulin Misfolding by Probes Derived from Functionalized Fluorene Frameworks.Molecules (Basel, Switzerland) · 2024Article
- Overview on the Polyphenol Avenanthramide in Oats (Nutrients · 2023Review
- Improving the Treatment Effect of Carotenoids on Alzheimer's Disease through Various Nano-Delivery Systems.International journal of molecular sciences · 2023Review
- NRF2 Activation by Nitrogen Heterocycles: A Review.Molecules (Basel, Switzerland) · 2023Review
- Article
- Neuroprotective effects of mild hypothermia against traumatic brain injury by the involvement of the Nrf2/ARE pathway.Brain and behavior · 2022Article
- Enantioselective Synthesis and Pharmacological Evaluation of Aza-CGP37157-Lipoic Acid Hybrids for the Treatment of Alzheimer's Disease.Antioxidants (Basel, Switzerland) · 2022Article
- Curcumin-Piperlongumine Hybrids with a Multitarget Profile Elicit Neuroprotection in In Vitro Models of Oxidative Stress and Hyperphosphorylation.Antioxidants (Basel, Switzerland) · 2021Article
- Melatonin Analogues Potently Inhibit MAO-B and Protect PC12 Cells against Oxidative Stress.Antioxidants (Basel, Switzerland) · 2021Article
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
Abstract
Oxidative stress is crucial to the outbreak and advancement of neurodegenerative diseases and is a common factor to many of them. We describe the synthesis of a library of derivatives of the 4-arylmethylen-2-pyrrolin-5-one framework by sequential application of a three-component reaction of primary amines, β-dicarbonyl compounds, and α-haloketones and a Knoevenagel condensation. These compounds can be viewed as cyclic amides of caffeic and ferulic acids, and are also structurally related to the bisavenanthramide family of natural antioxidants. Most members of the library showed low cytotoxicity and good activity as inductors of Nrf2, a transcription factor that acts as the master regulator of the antioxidant response associated with activation of the antioxidant response element (ARE). Nrf2-dependent protein expression was also proved by the significant increase in the levels of the HMOX1 and NQO1 proteins. Some compounds exerted neuroprotective properties in oxidative stress situations, such as rotenone/oligomycin-induced toxicity, and also against protein hyperphosphorylation induced by the phosphatase inhibitor okadaic acid. Compound
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