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Synthesis, anti-mycobacterial activity and DNA sequence-selectivity of a library of biaryl-motifs containing polyamides.
Brucoli, Federico; Guzman, Juan D; Maitra, Arundhati; James, Colin H; Fox, Keith R; Bhakta, Sanjib.
Afiliação
  • Brucoli F; School of Science and Sport, Institute of Biomedical and Environmental Health Research (IBEHR), University of the West of Scotland, Paisley PA1 2BE, UK. Electronic address: federico.brucoli@uws.ac.uk.
  • Guzman JD; Mycobacteria Research Laboratory, Department of Biological Sciences, The Institute of Structural and Molecular Biology, Birkbeck, University of London, London WC1E 7HX, UK.
  • Maitra A; Mycobacteria Research Laboratory, Department of Biological Sciences, The Institute of Structural and Molecular Biology, Birkbeck, University of London, London WC1E 7HX, UK.
  • James CH; UCL School of Pharmacy, London, 29-39 Brunswick Square, London WC1N 1AX, UK.
  • Fox KR; Centre for Biological Sciences, Life Sciences Building 85, University of Southampton, Southampton SO17 1BJ, UK.
  • Bhakta S; Mycobacteria Research Laboratory, Department of Biological Sciences, The Institute of Structural and Molecular Biology, Birkbeck, University of London, London WC1E 7HX, UK.
Bioorg Med Chem ; 23(13): 3705-11, 2015 Jul 01.
Article em En | MEDLINE | ID: mdl-25921267
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 Mycobacterium tuberculosis compared to distamycin and library member 2(5,7) showed high binding affinity for the 5'-ACATAT-3' sequence.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: DNA Bacteriano / Distamicinas / Bibliotecas de Moléculas Pequenas / Nylons / Antituberculosos Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: DNA Bacteriano / Distamicinas / Bibliotecas de Moléculas Pequenas / Nylons / Antituberculosos Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article