Abstract
Synthetic array technology was utilized to rapidly synthesize and analyze a diverse set of reductive alkylation analogues of daptomycin. Analysis of the array suggested the use of polar functionality such as sulfonamides or amide or polar spaces such as piperazine would beneficially affect activity.
MeSH terms
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Alkylation
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Amides / chemistry
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / pharmacology
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Combinatorial Chemistry Techniques
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Daptomycin / analogs & derivatives*
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Daptomycin / chemical synthesis*
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Daptomycin / pharmacology
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Drug Design
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Enterococcus faecalis / drug effects
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Enterococcus faecium / drug effects
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Lipids / chemistry*
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Microbial Sensitivity Tests
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Molecular Structure
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Oxidation-Reduction*
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Peptides, Cyclic / chemical synthesis*
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Peptides, Cyclic / pharmacology
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Piperazine
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Piperazines / chemistry
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Staphylococcus aureus / drug effects
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Structure-Activity Relationship
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Sulfonamides / chemistry
Substances
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Amides
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Anti-Bacterial Agents
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Lipids
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Peptides, Cyclic
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Piperazines
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Sulfonamides
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Piperazine
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Daptomycin