Title Synthesis of novel aminothiazole derivatives as promising antiviral, antioxidant and antibacterial candidates /
Authors Minickaitė, Rūta ; Grybaitė, Birutė ; Vaickelionienė, Rita ; Kavaliauskas, Povilas ; Petraitis, Vidmantas ; Petraitienė, Rūta ; Tumosienė, Ingrida ; Jonuškienė, Ilona ; Mickevičius, Vytautas
DOI 10.3390/ijms23147688
Full Text Download
Is Part of International journal of molecular sciences.. Basel : MDPI. 2022, vol. 23, iss. 14, art. no. 7688, p. 1-19.. ISSN 1661-6596. eISSN 1422-0067
Keywords [eng] thiazole ; antiviral ; oxidative stress ; antioxidant ; antibacterial ; bioactivity
Abstract [eng] 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.
Published Basel : MDPI
Type Journal article
Language English
Publication date 2022
CC license CC license description