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DNA binding ligands targeting drug-resistant Gram-positive bacteria. Part 1: Internal benzimidazole derivatives
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
Affiliation:Genesoft Pharmaceuticals Inc., 7300 Shoreline Court, South San Francisco, CA 94080, USA.
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).
Keywords:
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