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 but also identified that the hydroxyl group at C-10 was essential for antibacterial activities.
Institute of Biotechnology and Pharmaceutical Research and ‡National Institute of Infectious Diseases and Vaccinology, National Health Research Institutes , Miaoli County 35053, Taiwan, R.O.C.
Jing-Kai
JK
Huang
Institute of Biotechnology and Pharmaceutical Research and ‡National Institute of Infectious Diseases and Vaccinology, National Health Research Institutes , Miaoli County 35053, Taiwan, R.O.C.
Tsai-Ling
TL
Yang Lauderdale
Institute of Biotechnology and Pharmaceutical Research and ‡National Institute of Infectious Diseases and Vaccinology, National Health Research Institutes , Miaoli County 35053, Taiwan, R.O.C.
Kak-Shan
KS
Shia
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011083:Polycyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D011083:Polycyclic Compounds; C581112:tetarimycin A