Abstract
Making use of the Hauser-Kraus annulation as a key step, the first total synthesis of tetarimycin A has been accomplished in a highly convergent and operationally simple manner. Preliminary SAR not only validated that tetarimycin A exhibited potent activity against MRSA and VRE at a low MIC value but also identified that the hydroxyl group at C-10 was essential for antibacterial activities.
Publication types
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Research Support, Non-U.S. Gov't
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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Methicillin-Resistant Staphylococcus aureus / drug effects*
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Microbial Sensitivity Tests
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Molecular Structure
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Polycyclic Compounds / chemical synthesis*
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Polycyclic Compounds / chemistry
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Polycyclic Compounds / pharmacology*
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Polycyclic Compounds
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tetarimycin A