Abstract
In this study, we report the design, synthesis and structure-activity relationships of novel indazole derivatives as DNA gyrase inhibitors with Gram-positive antibacterial activity. Our results show that selected compounds from this series exhibit potent antibacterial activity against Gram-positive bacteria including multi-drug resistant strains that is methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VRE).
MeSH terms
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / pharmacology
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DNA Topoisomerases / drug effects
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Drug Design
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Drug Resistance, Multiple
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Enterococcus faecalis / drug effects
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Enterococcus faecalis / enzymology
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology
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Gram-Positive Bacteria / drug effects*
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Gram-Positive Bacteria / enzymology
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Humans
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Imidazoles / chemical synthesis
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Imidazoles / pharmacology*
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Inhibitory Concentration 50
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Microbial Sensitivity Tests
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Staphylococcaceae / drug effects
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Staphylococcaceae / enzymology
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Structure-Activity Relationship
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Topoisomerase II Inhibitors*
Substances
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Anti-Bacterial Agents
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Enzyme Inhibitors
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Imidazoles
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Topoisomerase II Inhibitors
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DNA Topoisomerases