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Design and Synthesis of π-Extended Resveratrol Analogues and In Vitro Antioxidant and Anti-Inflammatory Activity Evaluation

The research on resveratrol ( ) has been conducted intensively over a long time due to its proven antioxidant activity and disease-fighting capabilities. Many efforts have also been made to increase these biological effects. In the present study, six new extended aromatic resveratrol analogues conta...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2021-01, Vol.26 (3), p.646
Main Authors: Nam, Ki Yoon, Damodar, Kongara, Lee, Yeontaek, Park, Lee Seul, Gim, Ji Geun, Park, Jae Phil, Jeon, Seong Ho, Lee, Jeong Tae
Format: Article
Language:English
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Summary:The research on resveratrol ( ) has been conducted intensively over a long time due to its proven antioxidant activity and disease-fighting capabilities. Many efforts have also been made to increase these biological effects. In the present study, six new extended aromatic resveratrol analogues containing naphthalene ( ) and its bioisosteres quinoline ( and ), isoquinoline ( ) quinoxaline ( ) and quinazoline ( ) scaffolds were designed and synthesized using an annulation strategy. The antioxidant and anti-inflammatory activities of these compounds were investigated. All compounds showed better antioxidant activity than resveratrol in ABTS assay. As for the anti-inflammatory test, and exhibited better activity than resveratrol. It is worth noting that nitrogen substitution on the extended aromatic resveratrol analogues has a significant impact on cell viability. Taking the antioxidant activities and NO inhibition activities into consideration, we conclude that isoquinoline analogue may qualify for the further investigation of antioxidant and anti-inflammatory therapy. Furthermore, our study results suggest that in order to improve the biological activity of polyphenolic compounds, extended aromaticity and nitrogen substitution strategy could be a viable method for the design of future drug candidates.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26030646