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  • Synthesis and structure-activity relationship study of novel quinazolinone-based inhibitors of MurA
    Hrast, Martina ...
    MurA is an intracellular bacterial enzyme that is essential for peptidoglycan biosynthesis, and is therefore an important target for antibacterial drug discovery. We report the synthesis, in silico ... studies and extensive structure-activity relationships of a series of quinazolinone-based inhibitors of MurA from Escherichia coli. 3-Benzyloxyphenylquinazolinones showed promising inhibitory potencies against MurA, in the low micromolar range, with an IC50 of 8 mM for the most potent derivative (58). Furthermore, furan-substituted quinazolinones (38, 46) showed promising antibacterial activities, with MICs from 1 mg/mL to 8 mg/mL, concomitant with their MurA inhibitory potencies. These data represent an important step towards the development of novel antimicrobial agents to combat increasing bacterial resistance.
    Source: Bioorganic & Medicinal Chemistry Letters. - ISSN 0960-894X (Vol. 27, iss. 15, 2017, str. 3529-3533)
    Type of material - article, component part ; adult, serious
    Publish date - 2017
    Language - english
    COBISS.SI-ID - 4336241

    Link(s):

    http://www.sciencedirect.com/science/article/pii/S0960894X17305620
    DOI

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