DNA Binding Ligands with Excellent Antibiotic Potency Against Drug-Resistant Gram-Positive Bacteria

An efficient synthesis of DNA binding molecules consisting of four heterocyclic carboxamide units and various substituents at both termini is described. The minor-groove binding ligands showed excellent activity against a broad range of Gram-positive bacteria; no cross-resistance to known antibacter...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-09, Vol.12 (18), p.2591-2594
Main Authors: Bürli, Roland W., Ge, Yigong, White, Sarah, Baird, Eldon E., Touami, Sofia M., Taylor, Matthew, Kaizerman, Jacob A., Moser, Heinz E.
Format: Article
Language:English
Subjects:
Amides - metabolism
Amides - pharmacology
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
DNA - metabolism
Drug Resistance, Microbial
Gram-Positive Bacteria - drug effects
Ligands
Medical sciences
Pharmacology. Drug treatments
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Summary:An efficient synthesis of DNA binding molecules consisting of four heterocyclic carboxamide units and various substituents at both termini is described. The minor-groove binding ligands showed excellent activity against a broad range of Gram-positive bacteria; no cross-resistance to known antibacterial drugs was observed. An efficient synthesis of DNA binding molecules consisting of four heterocyclic carboxamide units and various substituents at both termini is described. The minor-groove binding ligands showed excellent activity against a broad range of Gram-positive bacteria; no cross-resistance to known antibacterial drugs was observed.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00515-2