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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Bibliographic Details
Published in:Organic letters 2015-09, Vol.17 (17), p.4248-4251
Main Authors: Huang, Jing-Kai, Yang Lauderdale, Tsai-Ling, Shia, Kak-Shan
Format: Article
Language:English
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
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Summary: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.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.5b02039