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    Synthesis of Novel Aminothiazole Derivatives as Promising Antiviral, Antioxidant and Antibacterial Candidates.

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    Author
    Minickaitė, Rūta
    Grybaitė, Birutė
    Vaickelionienė, Rita
    Kavaliauskas, Povilas
    Petraitis, Vidmantas
    Petraitienė, Rūta
    Tumosienė, Ingrida
    Jonuškienė, Ilona
    Mickevičius, Vytautas
    Date
    2022-07-12
    Journal
    International Journal of Molecular Sciences
    Publisher
    MDPI AG
    Type
    Article
    
    Metadata
    Show full item record
    See at
    https://doi.org/10.3390/ijms23147688
    Abstract
    It is well-known that thiazole derivatives are usually found in lead structures, which demonstrate a wide range of pharmacological effects. The aim of this research was to explore the antiviral, antioxidant, and antibacterial activities of novel, substituted thiazole compounds and to find potential agents that could have biological activities in one single biomolecule. A series of novel aminothiazoles were synthesized, and their biological activity was characterized. The obtained results were compared with those of the standard antiviral, antioxidant, antibacterial and anticancer agents. The compound bearing 4-cianophenyl substituent in the thiazole ring demonstrated the highest cytotoxic properties by decreasing the A549 viability to 87.2%. The compound bearing 4-trifluoromethylphenyl substituent in the thiazole ring showed significant antiviral activity against the PR8 influenza A strain, which was comparable to the oseltamivir and amantadine. Novel compounds with 4-chlorophenyl, 4-trifluoromethylphenyl, phenyl, 4-fluorophenyl, and 4-cianophenyl substituents in the thiazole ring demonstrated antioxidant activity by DPPH, reducing power, FRAP methods, and antibacterial activity against Escherichia coli and Bacillus subtilis bacteria. These data demonstrate that substituted aminothiazole derivatives are promising scaffolds for further optimization and development of new compounds with potential influenza A-targeted antiviral activity. Study results could demonstrate that structure optimization of novel aminothiazole compounds may be useful in the prevention of reactive oxygen species and developing new specifically targeted antioxidant and antibacterial agents.
    Keyword
    antibacterial
    antioxidant
    antiviral
    bioactivity
    oxidative stress
    thiazole
    Identifier to cite or link to this item
    http://hdl.handle.net/10713/19498
    ae974a485f413a2113503eed53cd6c53
    10.3390/ijms23147688
    Scopus Count
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