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 antibacterial drugs was observed.
Bürli
Roland W
RW
Genesoft Inc, 7300 Shoreline Court, South San Francisco, CA 94080, USA. rburli@genesoft.com
Ge
Yigong
Y
White
Sarah
S
Baird
Eldon E
EE
Touami
Sofia M
SM
Taylor
Matthew
M
Kaizerman
Jacob A
JA
Moser
Heinz E
HE
D000577:Amides / Q000378:metabolism / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D004247:DNA / Q000378:metabolism*; D004352:Drug Resistance, Microbial; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008024:Ligands
D000577:Amides; D000900:Anti-Bacterial Agents; D008024:Ligands; D004247:DNA