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Studies on Antibiotics Active against Resistant Bacteria. Total Synthesis of MRSA-Active Tetarimycin A and Its Analogues

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 bu...

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Published in:Organic letters 2015-09, Vol.17 (17), p.4248-4251
Main Authors: Huang, Jing-Kai, Yang Lauderdale, Tsai-Ling, Shia, Kak-Shan
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Language:English
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cited_by cdi_FETCH-LOGICAL-a345t-ff38560fc965fe2ad980baa3dcc33b28f34b46d90b5252fe4b6a02b1377405493
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description 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.
doi_str_mv 10.1021/acs.orglett.5b02039
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source American Chemical Society:Jisc Collections:American Chemical Society Read & Publish Agreement 2022-2024 (Reading list)
subjects Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Methicillin-Resistant Staphylococcus aureus - drug effects
Microbial Sensitivity Tests
Molecular Structure
Polycyclic Compounds - chemical synthesis
Polycyclic Compounds - chemistry
Polycyclic Compounds - pharmacology
Structure-Activity Relationship
title Studies on Antibiotics Active against Resistant Bacteria. Total Synthesis of MRSA-Active Tetarimycin A and Its Analogues
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