Abstract
Starting from a biased needle screening hit 3a, we report herein the design and synthesis of a series of novel 2,3-dihydroisoindol-1-ones structurally related to cyclothialidine 2 with DNA gyrase inhibitory activity. In this series, some compounds exhibited promising antibacterial activity against gram-positive bacterial strains.
MeSH terms
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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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Drug Design*
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Molecular Structure
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Phenols / chemistry*
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Phenols / pharmacology*
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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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Phenols
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Topoisomerase II Inhibitors