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  • Synthesis and biological evaluation of new glutamic acid-based inhibitors of MurD ligase
    Tomašič, Tihomir ...
    Mur ligases catalyze the biosynthesis of the UDP-MurNAc-pentapeptide precursorof peptidoglycan, an essential polymer of bacterial cell-wall. They constitute attractive targets for the development of ... novel antibacterial agents. Here we report on the synthesis of a series of 2,4-diaminoquinazolines, quinazoline- 2,4(1H,3H)-diones, 5-benzylidenerhodanines and 5-benzylidenethiazolidine-2,4-diones and their inhibitory activities against MurD from Escherichia coli. Compounds (R)-27 and(S)-27 showed inhibitory activity against MurD with IC50 values of 174 and 206 lM, respectively, which makes them promising starting points for optimization.
    Source: Bioorganic & Medicinal Chemistry Letters. - ISSN 0960-894X (Vol. 19, no. 1, 2009, str. 153-157)
    Type of material - article, component part
    Publish date - 2009
    Language - english
    COBISS.SI-ID - 2485361