Formal Single Atom Editing of the Glycosylated Natural Product Fidaxomicin Improves Acid Stability and Retains Antibiotic Activity
Isabella Ferrara,
Gleb A. Chesnokov,
Silvia Dittmann
et al.
Abstract:Fidaxomicin (Fdx) constitutes a glycosylated natural
product with
excellent antibacterial activity against various Gram-positive bacteria
but is approved only for Clostridioides difficile infections. Poor water solubility and acid lability preclude its
use for other infections. Herein, we describe our strategy to overcome
the acid lability by introducing acid-stable S-linked glycosides.
We describe the direct, diastereoselective modification of unprotected
Fdx without the need to avoid air or moisture. Using o… Show more
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