| Literature DB >> 25921267 |
Federico Brucoli1, Juan D Guzman2, Arundhati Maitra2, Colin H James3, Keith R Fox4, Sanjib Bhakta2.
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.Entities:
Keywords: Anti-tubercular agents; Antibiotic resistance; Combinatorial chemistry; DNA-minor groove ligands; Distamycin; Whole cell phenotypic evaluation
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Year: 2015 PMID： 25921267 DOI： 10.1016/j.bmc.2015.04.001
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641