Abstract
Amidino benzimidazoles have been identified as inhibitors of the bacterial KinA/Spo0F two-component system (TCS). Many of these inhibitors exhibit good in vitro antibacterial activity against a variety of susceptible and resistant Gram-positive organisms. The moiety at the 2-position of the benzimidazole was extensively modified. In addition, the regioisomeric benzoxazoles, heterocyclic replacements for the benzimidazole, have been synthesized and their activity against the TCS evaluated.
MeSH terms
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Amidines / chemical synthesis
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Amidines / pharmacology
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / pharmacology
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Bacterial Proteins / antagonists & inhibitors
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Benzimidazoles / chemical synthesis
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Benzimidazoles / pharmacology*
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Combinatorial Chemistry Techniques
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Gram-Positive Bacteria / drug effects*
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Gram-Positive Bacteria / physiology
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Inhibitory Concentration 50
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Microbial Sensitivity Tests
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Protein Kinase Inhibitors
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Protein Kinases*
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Signal Transduction / drug effects
Substances
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Amidines
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Anti-Bacterial Agents
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Bacterial Proteins
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Benzimidazoles
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Protein Kinase Inhibitors
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Spo0F protein, Bacillus subtilis
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kinA protein, Bacillus subtilis
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Protein Kinases