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  • Ellipticines and 9-acridinylamines as inhibitors of d-alanine : d-alanine ligase
    Vehar, Blaž ...
    D-alanine: D-alanine ligase (Ddl), an intracellular bacterial enzyme essential for cell wall biosynthesis, is an attractive target for development of novel antimicrobial drugs. This study focused on ... an extensive evaluation of two families of Ddl inhibitors encountered in our previous research. New members of both families were obtained through similarity search and synthesis. Ellipticines and 9-acridinylamines were both found to possess inhibitory activity against Ddl from E. coli and antimicrobial activity against E. coli and S. aureus. Ellipticines with a quaternary methylpyridinium moiety were themost potent among all studied compounds, with MIC values as low as 2 mg/L in strains with intact efflux mechanisms. Antimicrobial activity of the studied compounds was connected to membrane damage, making their development as antibacterial drug candidates unlikely unless analogues devoid of this nonspecific effect can be discovered.
    Source: Bioorganic & Medicinal Chemistry. - ISSN 0968-0896 (Vol. 19, issue 17, 2011, str. 5137-5146)
    Type of material - article, component part
    Publish date - 2011
    Language - english
    COBISS.SI-ID - 4728346
    DOI

source: Bioorganic & Medicinal Chemistry. - ISSN 0968-0896 (Vol. 19, issue 17, 2011, str. 5137-5146)
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