title: 6-oxa isosteres of anacardic acids as potent inhibitors of bacterial histidine protein kinase (HPK)-mediated two-component regulatory systems.
abstract: A series of 6-oxa isosteres of anacardic acids (6-higher alkyl/alkenyl-2-hydroxybenzoic acids) was synthesised and several members were discovered to be among the most potent inhibitors (IC50 values < or = 5 microM) of the bacterial two-component regulatory systems, KinA/SpoOF and NRII/NRI, reported to date. The Gram-positive antibacterial activity in selected strains is also presented.
authors.affiliation: The R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869-0602, USA.
authors.forename: R M
authors.initials: RM
authors.lastname: Kanojia
authors.forename: W
authors.initials: W
authors.lastname: Murray
authors.forename: J
authors.initials: J
authors.lastname: Bernstein
authors.forename: J
authors.initials: J
authors.lastname: Fernandez
authors.forename: B D
authors.initials: BD
authors.lastname: Foleno
authors.forename: H
authors.initials: H
authors.lastname: Krause
authors.forename: L
authors.initials: L
authors.lastname: Lawrence
authors.forename: G
authors.initials: G
authors.lastname: Webb
authors.forename: J F
authors.initials: JF
authors.lastname: Barrett
mesh_terms: D048729:Anacardic Acids; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000201:enzymology*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D000071677:Histidine Kinase; D008826:Microbial Sensitivity Tests; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases / Q000378:metabolism; D012459:Salicylates / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D048729:Anacardic Acids; D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D047428:Protein Kinase Inhibitors; D012459:Salicylates; C088115:anacardic acid; D011494:Protein Kinases; D000071677:Histidine Kinase