Synthesis and Biological Activity of Thiazolyl-Acetic Acid Derivatives as Possible Antimicrobial Agents

DOI PubMed 被引用文献2件 参考文献40件
  • SHIRAI AKIHIRO
    Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima
  • FUMOTO YASUKO
    Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima
  • SHOUNO TOMOAKI
    Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima
  • MASEDA HIDEAKI
    Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima
  • OMASA TAKESHI
    Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima Department of Biological Science and Technology, Biosystems Engineering, Institute of Technology and Science, The University of Tokushima

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5a-h, a series of (5-substituted-2-methyl-1,3-thiazole-4-yl) acetic acids as heterocyclic acetic acid derivatives, was designed and synthesized from ethyl acetoacetate. The synthesized compounds were screened for their antimicrobial activities against bacterial and fungal strains, and their characteristics were investigated by assays under various temperature and pH conditions. Cytotoxicity was evaluated with the use of sheep erythrocytes and human neonate dermal fibroblasts. Similarly, agents such as lauric acid 6 and parabens 7a-b, which are used as preservative agents for commercial cosmetics and detergents, were assayed for comparison. Although the structure of 5a is simple, comprising a thiazole attached with an octyl group and acetic acid moiety, the compound showed stronger and broader antibacterial and antifungal activities among the 5 series against the tested microbes other than gram-negative bacteria. Interestingly, 5a overcame the weak antifungal activity of parabens 7a-b. Also, the cytotoxicity of 5a was less than that of parabens 7a-b, especially to human dermal fibroblasts. These results suggest that thiazolyl-acetic acid 5a is a potentially effective biocide, and that it could be used as a preservative agent in commercially sold cosmetics and detergents, facilitated by the hydrophilic and charge properties of its carboxylic acid moiety.

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