Bioactive fluorinated derivative of amphotericin B

Bioorganic & Medicinal Chemistry Letters
2005.0

Abstract

The first stably fluorinated derivative of amphotericin B2 with a fluorine atom in the macrolide skeleton was synthesized using an electrophilic fluorination reagent, Selectfluor. The derivative 2 showed hemolytic, K+ permeable, and antifungal activities similar to those of AmB and thus was expected to be a powerful tool for NMR-based investigations on the mechanism of ion-channel formation by amphotericin B.

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