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 Faculties and Schools > Faculty of Science > School of Natural Sciences |
| Research Centres and Institutes: | Structural Molecular Biology, Institute of (ISMB) |
| Depositing User: | Administrator |
| Date Deposited: | 21 Apr 2015 07:48 |
| Last Modified: | 02 Aug 2023 17:15 |
| URI: | https://eprints.bbk.ac.uk/id/eprint/11950 |
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