Abstract
Background: Antioxidants are developed to assist the immune system and overcome oxidative stress, the aggression of cellular constituents due to imbalance between reactive oxygen species and the inner antioxidant system. The main objective of this study was to search for new and potent antioxidants to protect humans against diseases associated with oxidative stress. Methods: In this study, three pyrano-[2,3-c]-pyrazole derivatives were synthesized via Multicomponent Reaction (MCR) approach and were characterized, using a melting point, High-Performance Liquid Chromatography (HPLC), and spectroscopic analyses (IR; 1H-NMR; 13C-NMR). All of the generated compounds were screened for their antioxidant properties in vivo, using ciliate “Tetrahymena” as a model organism exposed to oxidative and nitrative stress. They were then studied in vitro by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays. Results: The results demonstrated that the three compounds (5a, b, c) are biologically active and possess potent antioxidant activities, especially the 5a and 5b derivatives. On the other hand, the in vitro bioassays revealed that the 5a derivative possessed a significant antioxidant activity much greater than ascorbic acid. Accordingly, the in silico data are consistent with the experimental data. Conclusion: These findings confirmed the potent antioxidant property of the synthesized compounds, providing us with new inspiration and challenges to design a library of pharmaceutical compounds with strong activity and low toxicity in the future.
Highlights
N owadays, a variety of antioxidant supplements have been developed to support the immune system and overcome oxidative stressors that are defined as the aggression of cellular constituents associated with an imbalance between reactive oxygen species and the body’s immune system [1]
A variety of antioxidants control the overproduction of free radicals within the human cells by inhibiting the oxidative stressors via various mechanisms
Characterization of the synthesized pyranopyrazoles: The analyses of the results shown in Table 1 demonstrated that the pyrano-[2,3-c]-pyrazoles were produced in good yields (93-95%), influenced by the nature of the substituent at the para position of the phenyl group
Summary
N owadays, a variety of antioxidant supplements have been developed to support the immune system and overcome oxidative stressors that are defined as the aggression of cellular constituents associated with an imbalance between reactive oxygen species and the body’s immune system [1]. Chief among powerful enzymatic and non-enzymatic antioxidants, there are Superoxide Dismutase (SOD), Catalase (CAT), Glutathione Peroxidase (GPx), and Glutathione-S-Transferase (GST) [4]. These enzymes maintain the balance between the pro- and anti-oxidant processes within the human cells. Antioxidants are developed to assist the immune system and overcome oxidative stress, the aggression of cellular constituents due to imbalance between reactive oxygen species and the inner antioxidant system. The main objective of this study was to search for new and potent antioxidants to protect humans against diseases associated with oxidative stress
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