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  • 5-benzylidenethiazolidin-4-ones as multitarget inhibitors of bacterial Mur ligases
    Tomašič, Tihomir ...
    Mur ligases participate in the intracellular path of bacterial peptidoglycan biosynthesis and constitute attractive, although so far underexploited, targets for antibacterial drug discovery. A series ... of hydroxy-substituted 5-benzylidenethiazolidin-4-ones were synthesized and tested as inhibitors of Mur ligases. The most potent compound 5 a was active against MurD-F with IC50 values between 2 and 6 m, making it a promising multitarget inhibitor of Mur ligases. Antibacterial activity against different strains, inhibitory activityagainst protein kinases, mutagenicity and genotoxicity of 5 a were also investigated, and kinetic and NMR studies were conducted.
    Source: ChemMedChem : Chemistry Enabling Drug Discovery. - ISSN 1860-7179 (Vol. 5, iss. 2, 2010, str. 286-295)
    Type of material - article, component part
    Publish date - 2010
    Language - english
    COBISS.SI-ID - 2743921

    Link(s):

    http://www3.interscience.wiley.com/journal/123218167/abstract

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