Semisynthetic Analogs of the Antibiotic Fidaxomicin – Design, Synthesis, and Biological Evaluation
2020
The glycoslated macrocyclic antibiotic fidaxomicin (1, tiacumicin B, lipiarmycin A3) displays good
to excellent activity against Gram-positive bacteria and was approved for the treatment of Clostridium difficile
infections (CDI). Main limitations of the compound include low water solubility, which impacts further clinical
use. We report on the synthesis of new fidaxomicin derivatives based on structural design and utilizing an
operationally simple one-step protecting group-free preparative approach from the natural product. An increase
in solubility of up to 25-fold with largely retained activity was observed. Furthermore, hybrid antibiotics were
prepared that show improved antibiotic activities
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