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  • New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold
    Pajk, Stane, 1983- ...
    Tetrahydropyran derivative 1 was discovered in a high-throughput screening campaign to find new inhibitors of mycobacterial InhA. Following initial in-vitro profiling, a structure-activity ... relationship study was initiated and a focused library of analogs was synthesized and evaluated. This yielded compound 42 with improved antimycobacterial activity and low cytotoxicity. Additionally, the crystal structure of InhA in complex with inhibitor 1 was resolved, to reveal the binding mode and provide hints for further optimization.
    Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 112, April 2016, str. 252-257)
    Type of material - article, component part ; adult, serious
    Publish date - 2016
    Language - english
    COBISS.SI-ID - 4025969

    Link(s):

    http://www.sciencedirect.com/science/article/pii/S0223523416300782

    Dostop preko računalnikov UL


    DOI

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