DNA binding ligands targeting drug-resistant Gram-positive bacteria. Part 1: Internal benzimidazole derivatives.
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).
Bürli
Roland W
RW
Genesoft Pharmaceuticals Inc., 7300 Shoreline Court, South San Francisco, CA 94080, USA.
McMinn
Dustin
D
Kaizerman
Jacob A
JA
Hu
Wenhao
W
Ge
Yigong
Y
Pack
Quinn
Q
Jiang
Vernon
V
Gross
Matthew
M
Garcia
Martin
M
Tanaka
Richard
R
Moser
Heinz E
HE
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D001562:Benzimidazoles / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D004247:DNA / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods*; D024881:Drug Resistance, Bacterial; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000502:physiology; D008024:Ligands; D051379:Mice; D011485:Protein Binding
D000900:Anti-Bacterial Agents; D001562:Benzimidazoles; D008024:Ligands; D004247:DNA