Abstract
This paper describes the discovery of alpha-trifluoroketoacetamides as potent antibacterial agents against Gram-positive organisms. The initial SAR indicates that the aryl ethyl side chain is essential in maintaining antibacterial activity. The SAR observations have been utilized to design a bioisostere for the alpha-trifluoroketoacetamide with good activity against Gram-positive organisms.
MeSH terms
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Acetamides / chemical synthesis
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Acetamides / pharmacology*
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / pharmacology*
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Fluoroacetates*
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Gram-Negative Bacteria / drug effects
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Gram-Positive Bacteria / drug effects*
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Microbial Sensitivity Tests
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Molecular Structure
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Structure-Activity Relationship
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Trifluoroacetic Acid / chemistry
Substances
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Acetamides
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Anti-Bacterial Agents
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Fluoroacetates
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trifluoroacetamide
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Trifluoroacetic Acid