6-Oxa isosteres of anacardic acids as potent inhibitors of bacterial histidine protein kinase (HPK)-mediated two-component regulatory systems

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 (IC 50 values ≤ 5 μM) of the bacterial two-component regulatory systems, KinA/SpoOF and NRII/NRI, reported to date...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 1999-10, Vol.9 (20), p.2947-2952
Hauptverfasser: Kanojia, Ramesh M., Murray, William, Bernstein, Jeffrey, Fernandez, Jeffrey, Foleno, Barbara D., Krause, Heather, Lawrence, Laura, Webb, Glenda, Barrett, John F.
Format: Artikel
Sprache:eng
Schlagworte:
Anacardic Acids
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Bacteria - enzymology
Biological and medical sciences
Enzyme Inhibitors - pharmacology
Histidine Kinase
Medical sciences
Microbial Sensitivity Tests
Pharmacology. Drug treatments
Protein Kinase Inhibitors
Protein Kinases - metabolism
Salicylates - chemistry
Salicylates - pharmacology
Structure-Activity Relationship
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Zusammenfassung: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 (IC 50 values ≤ 5 μM) 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. A series of 6-oxa isosteres 1 of anacardic acids (6-higher alkyl/alkenyl-2-hydroxybenzoic acids) was synthesised and several members were discovered to be among the most potent inhibitors (IC 50 values ≤ 5 μM) 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. [Display omitted]
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00508-9