4.5 Article

DNA binding ligands targeting drug-resistant gram-positive bacteria.: Part 1:: Internal benzimidazole derivatives

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 14, Issue 5, Pages 1253-1257

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2003.12.042

Keywords

antibiotics; DNA binders; minor groove; lead optimization

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Novel DNA minor-groove binding ligands with a promising antibacterial profile are described. Apart from excellent in vitro potency against multiple Gram-positive bacterial strains such as methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), and penicillin-intermediate Streptococcus pneumoniae (PISP), a small subset of compounds was active against Gram-negative bacteria such as Escherichia coli (E. coli). (C) 2003 Elsevier Ltd. All rights reserved.

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