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

Author

Huang JK, Yang Lauderdale TL, and Shia KS

Subjects
Anti-Bacterial Agents chemistry, Anti-Bacterial Agents pharmacology, Microbial Sensitivity Tests, Molecular Structure, Polycyclic Compounds chemistry, Structure-Activity Relationship, Anti-Bacterial Agents chemical synthesis, Methicillin-Resistant Staphylococcus aureus drug effects, Polycyclic Compounds chemical synthesis, Polycyclic Compounds pharmacology
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.

Published
2015
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