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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container_title	Bioorganic & medicinal chemistry letters
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creator	Kanojia, Ramesh M. Murray, William Bernstein, Jeffrey Fernandez, Jeffrey Foleno, Barbara D. Krause, Heather Lawrence, Laura Webb, Glenda Barrett, John F.
description	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]
doi_str_mv	10.1016/S0960-894X(99)00508-9
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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]</description><subject>Anacardic Acids</subject><subject>Anti-Bacterial Agents - chemistry</subject><subject>Anti-Bacterial Agents - pharmacology</subject><subject>Antibacterial agents</subject><subject>Antibiotics. Antiinfectious agents. 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subjects	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
title	6-Oxa isosteres of anacardic acids as potent inhibitors of bacterial histidine protein kinase (HPK)-mediated two-component regulatory systems
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