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

被引:15
作者
Minickaite, Ruta [1 ]
Grybaite, Birute [1 ]
Vaickelioniene, Rita [1 ]
Kavaliauskas, Povilas [1 ,2 ,3 ,4 ,5 ]
Petraitis, Vidmantas [2 ,4 ,5 ]
Petraitiene, Ruta [2 ,4 ]
Tumosiene, Ingrida [1 ]
Jonuskiene, Ilona [1 ]
Mickevicius, Vytautas [1 ]
机构
[1] Kaunas Univ Technol, Fac Chem Technol, Dept Organ Chem, Radvilenu Pl 19, LT-50254 Kaunas, Lithuania
[2] Cornell Univ, Div Infect Dis, Dept Med, Transplantat Oncol Infect Dis Program,Weill Corne, 527 East 68th St, New York, NY 10065 USA
[3] Univ Maryland Baltimore, Dept Microbiol & Immunol, Sch Med, 655 W Baltimore St, Baltimore, MD 21201 USA
[4] Inst Infect Dis & Pathogen Microbiol, Birstono Str 38A, LT-59116 Prienai, Lithuania
[5] Lithuanian Univ Hlth Sci, Vet Acad, Biol Res Ctr, Tilzes St 18, LT-47181 Kaunas, Lithuania
关键词
thiazole; antiviral; oxidative stress; antioxidant; antibacterial; bioactivity; THIAZOLE; CHEMISTRY;
D O I
10.3390/ijms23147688
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
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页数:19
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