Abstract
A series of simplified thiomarinol derivatives was prepared by way of catalytic enantioselective inverse electron demand hetero [4+2] cycloaddition/allylboration tandem reaction. As a preliminary evaluation, these analogs were tested for antimicrobial activity using a standard disk diffusion assay. Whereas amide analogs were less active, the simple ester analogs 3 and 4 were demonstrated to be more active than thiomarinol H.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acyl-tRNA Synthetases / antagonists & inhibitors
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Amino Acyl-tRNA Synthetases / metabolism
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / pharmacology
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Cyclization
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Disk Diffusion Antimicrobial Tests
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Mupirocin / analogs & derivatives
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Mupirocin / chemical synthesis
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Mupirocin / chemistry
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Mupirocin / pharmacology
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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thiomarinol
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Mupirocin
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Amino Acyl-tRNA Synthetases