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  • New 5-benzylidenethiazolidin-4-one inhibitors of bacterial MurD ligase: design, synthesis, crystal structures, and biological evaluation
    Zidar, Nace ...
    Mur ligases (MurCeMurF), a group of bacterial enzymes that catalyze four consecutive steps in the formation of cytoplasmic peptidoglycan precursor, are becoming increasingly adopted as targets in ... antibacterial drug design. Based on the crystal structure of MurD cocrystallized with thiazolidine-2,4- dione inhibitor I, we have designed, synthesized, and evaluated a series of improved glutamic acid containing 5-benzylidenerhodanine and 5-benzylidenethiazolidine-2,4-dione inhibitors of MurD with IC50 values up to 28 mM. Inhibitor 37, with an IC50 of 34 mM, displays a weak antibacterial activity against S. aureus ATCC 29213 and E. faecalis ATCC 29212 with minimal inhibitory concentrations of 128 mg/mL. High-resolution crystal structures of MurD in complex with two new inhibitors (compounds 23 and 51) reveal details of their binding modes within the active site and provide valuable information for further structure-based optimization.
    Vir: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 46, issue 11, 2011, str. 5512-5523)
    Vrsta gradiva - članek, sestavni del
    Leto - 2011
    Jezik - angleški
    COBISS.SI-ID - 3107953

    Povezava(-e):

    http://www.sciencedirect.com/science/article/pii/S0223523411006775
    http://www.sciencedirect.com/science/journal/aip/02235234
    DOI

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