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.