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Synthesis of Novel Aminothiazole Derivatives as Promising Antiviral, Antioxidant and Antibacterial Candidates.
Minickaite, Ruta; Grybaite, Birute; Vaickelioniene, Rita; Kavaliauskas, Povilas; Petraitis, Vidmantas; Petraitiene, Ruta; Tumosiene, Ingrida; Jonuskiene, Ilona; Mickevicius, Vytautas.
  • Minickaite R; Department of Organic Chemistry, Faculty of Chemical Technology, Kaunas University of Technology, Radvilenu pl. 19, LT-50254 Kaunas, Lithuania.
  • Grybaite B; Department of Organic Chemistry, Faculty of Chemical Technology, Kaunas University of Technology, Radvilenu pl. 19, LT-50254 Kaunas, Lithuania.
  • Vaickelioniene R; Department of Organic Chemistry, Faculty of Chemical Technology, Kaunas University of Technology, Radvilenu pl. 19, LT-50254 Kaunas, Lithuania.
  • Kavaliauskas P; Department of Organic Chemistry, Faculty of Chemical Technology, Kaunas University of Technology, Radvilenu pl. 19, LT-50254 Kaunas, Lithuania.
  • Petraitis V; Transplantation-Oncology Infectious Diseases Program, Division of Infectious Diseases, Department of Medicine, Weill Cornell Medicine of Cornell University, 527 East 68th Street, New York, NY 10065, USA.
  • Petraitiene R; Department of Microbiology and Immunology, University of Maryland Baltimore School of Medicine, 655 W. Baltimore Street, Baltimore, MD 21201, USA.
  • Tumosiene I; Institute of Infectious Diseases and Pathogenic Microbiology, Birstono Str. 38A, LT-59116 Prienai, Lithuania.
  • Jonuskiene I; Biological Research Center, Veterinary Academy, Lithuanian University of Health Sciences, Tilzes St. 18, LT-47181 Kaunas, Lithuania.
  • Mickevicius V; Transplantation-Oncology Infectious Diseases Program, Division of Infectious Diseases, Department of Medicine, Weill Cornell Medicine of Cornell University, 527 East 68th Street, New York, NY 10065, USA.
Int J Mol Sci ; 23(14)2022 Jul 12.
Article in English | MEDLINE | ID: covidwho-1964004
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.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Influenza, Human / Antioxidants Limits: Humans Language: English Year: 2022 Document Type: Article Affiliation country: Ijms23147688

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Influenza, Human / Antioxidants Limits: Humans Language: English Year: 2022 Document Type: Article Affiliation country: Ijms23147688