Abstract
Platensimycin (1) displays antibacterial activity due to its inhibition of the elongation condensing enzyme (FabF), a novel mode of action that could potentially lead to a breakthrough in developing a new generation of antibiotics. The medicinal chemistry efforts were focused on the modification of the enone moiety of platensimycin and several analogs showed significant activity against FabF and possess antibacterial activity.
MeSH terms
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3-Oxoacyl-(Acyl-Carrier-Protein) Synthase / antagonists & inhibitors*
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3-Oxoacyl-(Acyl-Carrier-Protein) Synthase / chemistry
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Adamantane / chemical synthesis*
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Adamantane / pharmacology
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Aminobenzoates / chemical synthesis*
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Aminobenzoates / pharmacology
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Anilides / chemical synthesis*
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Anilides / 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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Bacterial Proteins / chemistry
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Chemistry, Pharmaceutical / methods*
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Crystallography, X-Ray / methods
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Drug Design
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Drug Resistance, Microbial
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Enterococcus faecalis / metabolism
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Inhibitory Concentration 50
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Methicillin / pharmacology
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Microbial Sensitivity Tests
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Models, Chemical
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Molecular Structure
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Streptomyces / metabolism
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Structure-Activity Relationship
Substances
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Aminobenzoates
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Anilides
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Anti-Bacterial Agents
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Bacterial Proteins
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3-Oxoacyl-(Acyl-Carrier-Protein) Synthase
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FabF protein, Enterococcus faecalis
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Adamantane
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platensimycin
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Methicillin