6-oxa isosteres of anacardic acids as potent inhibitors of bacterial histidine protein kinase (HPK)-mediated two-component regulatory systems.
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.
Kanojia
R M
RM
The R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869-0602, USA.
Murray
W
W
Bernstein
J
J
Fernandez
J
J
Foleno
B D
BD
Krause
H
H
Lawrence
L
L
Webb
G
G
Barrett
J F
JF
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
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