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    Synthesis of novel thiazole derivatives bearing β-amino acid and aromatic moieties as promising scaffolds for the development of new antibacterial and antifungal candidates targeting multidrug-resistant pathogens

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    Author
    Malūkaitė, Dovilė
    Grybaitė, Birutė
    Vaickelionienė, Rita
    Vaickelionis, Giedrius
    Sapijanskaitė-Banevič, Birutė
    Kavaliauskas, Povilas
    Mickevičius, Vytautas
    Date
    2022-01-01
    Journal
    Molecules (Basel, Switzerland)
    Publisher
    MDPI AG
    Type
    Article
    
    Metadata
    Show full item record
    See at
    https://doi.org/10.3390/molecules27010074
    Abstract
    Rapidly growing antimicrobial resistance among clinically important bacterial and fungal pathogens accounts for high morbidity and mortality worldwide. Therefore, it is critical to look for new small molecules targeting multidrug-resistant pathogens. Herein, in this paper we report a synthesis, ADME properties, and in vitro antimicrobial activity characterization of novel thiazole derivatives bearing β-amino acid, azole, and aromatic moieties. The in silico ADME characterization revealed that compounds 1–9 meet at least 2 Lipinski drug-like properties while cytotoxicity studies demonstrated low cytotoxicity to Vero cells. Further in vitro antimicrobial activity characterization showed the selective and potent bactericidal activity of 2a–c against Gram-positive pathogens (MIC 1–64 µg/mL) with profound activity against S. aureus (MIC 1–2 µg/mL) harboring genetically defined resistance mechanisms. Furthermore, the compounds 2a–c exhibited antifungal activity against azole resistant A. fumigatus, while only 2b and 5a showed antifungal activity against multidrug resistant yeasts including Candida auris. Collectively, these results demonstrate that thiazole derivatives 2a–c and 5a could be further explored as a promising scaffold for future development of antifungal and antibacterial agents targeting highly resistant pathogenic microorganisms. © 2021 by the authors.
    Keyword
    Antimicrobial activity
    Azole
    Thiazoles
    β-amino acids
    Identifier to cite or link to this item
    http://hdl.handle.net/10713/17600
    ae974a485f413a2113503eed53cd6c53
    10.3390/molecules27010074
    Scopus Count
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