DNA binding ligands targeting drug-resistant Gram-positive bacteria. Part 1: Internal benzimidazole derivatives |
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Authors: | Bürli Roland W McMinn Dustin Kaizerman Jacob A Hu Wenhao Ge Yigong Pack Quinn Jiang Vernon Gross Matthew Garcia Martin Tanaka Richard Moser Heinz E |
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Affiliation: | Genesoft Pharmaceuticals Inc., 7300 Shoreline Court, South San Francisco, CA 94080, USA. |
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Abstract: | ![]() 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). |
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