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    Synthesis, anti-mycobacterial activity and DNA sequence-selectivity of a library of biaryl-motifs containing polyamides

    Brucoli, F. and Guzman, Juan D. and Maitra, Arundhati and James, C.H. and Fox, K.R. and Bhakta, Sanjib (2015) Synthesis, anti-mycobacterial activity and DNA sequence-selectivity of a library of biaryl-motifs containing polyamides. Bioorganic & Medicinal Chemistry 23 (13), pp. 3705-3711. ISSN 0968-0896.

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    Abstract

    The alarming rise of extensively drug-resistant tuberculosis (XDR-TB) strains, compel the development of new molecules with novel modes of action to control this world health emergency. Distamycin analogues containing N-terminal biaryl-motifs 2(1-5)(1-7) were synthesised using a solution-phase approach and evaluated for their anti-mycobacterial activity and DNA-sequence selectivity. Thiophene dimer motif-containing polyamide 2(2,6) exhibited 10-fold higher inhibitory activity against M. tuberculosis compared to distamycin and library member 2(5,7) showed high binding affinity for the 5’-ACATAT-3’ sequence.

    Metadata

    Item Type: Article
    Keyword(s) / Subject(s): Distamycin, Antibiotic resistance, Anti-tubercular agents, DNA-minor groove ligands, Whole cell phenotypic evaluation, Combinatorial chemistry
    School: Birkbeck Schools and Departments > School of Science > Biological Sciences
    Research Centre: Structural Molecular Biology, Institute of (ISMB)
    Depositing User: Administrator
    Date Deposited: 21 Apr 2015 07:48
    Last Modified: 29 Jul 2019 16:07
    URI: http://eprints.bbk.ac.uk/id/eprint/11950

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