title: DNA binding ligands with in vivo efficacy in murine models of bacterial infection: optimization of internal aromatic amino acids.
abstract: DNA binding ligands with potent antimicrobial activity against Gram-positive bacteria were further optimized by variation of the internal aromatic amino acids. This modification led to compounds with improved in vivo efficacy in lethal murine models of peritonitis (methicillin-resistant S. aureus, MRSA) and lung infection (S. pneumoniae).
authors.affiliation: Genesoft Pharmaceuticals, 7300 Shoreline Court, South San Francisco, CA 94080, USA.
authors.forename: Roland W
authors.initials: RW
authors.lastname: Bürli
authors.forename: Jacob A
authors.initials: JA
authors.lastname: Kaizerman
authors.forename: Jian-Xin
authors.initials: JX
authors.lastname: Duan
authors.forename: Peter
authors.initials: P
authors.lastname: Jones
authors.forename: Kirk W
authors.initials: KW
authors.lastname: Johnson
authors.forename: Mari
authors.initials: M
authors.lastname: Iwamoto
authors.forename: Kiet
authors.initials: K
authors.lastname: Truong
authors.forename: Wenhao
authors.initials: W
authors.lastname: Hu
authors.forename: Timothy
authors.initials: T
authors.lastname: Stanton
authors.forename: Alfred
authors.initials: A
authors.lastname: Chen
authors.forename: Sofia
authors.initials: S
authors.lastname: Touami
authors.forename: Matthew
authors.initials: M
authors.lastname: Gross
authors.forename: Vernon
authors.initials: V
authors.lastname: Jiang
authors.forename: Yigong
authors.initials: Y
authors.lastname: Ge
authors.forename: Heinz E
authors.initials: HE
authors.lastname: Moser
mesh_terms: D024322:Amino Acids, Aromatic / Q000737:chemistry*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000378:metabolism / Q000494:pharmacology*; D004247:DNA / Q000378:metabolism*; D004195:Disease Models, Animal; D008024:Ligands; D008171:Lung Diseases / Q000188:drug therapy / Q000382:microbiology; D051379:Mice; D010538:Peritonitis / Q000188:drug therapy / Q000382:microbiology; D013203:Staphylococcal Infections / Q000188:drug therapy* / Q000382:microbiology; D013211:Staphylococcus aureus / Q000302:isolation & purification; D013290:Streptococcal Infections / Q000188:drug therapy* / Q000382:microbiology; D013296:Streptococcus pneumoniae / Q000302:isolation & purification
chemical_list: D024322:Amino Acids, Aromatic; D000900:Anti-Bacterial Agents; D008024:Ligands; D004247:DNA