title: Bioactive fluorinated derivative of amphotericin B.
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.
authors.affiliation: Department of Chemistry, Graduate School of Science, Osaka University, Toyonaka, Osaka 560-0043, Japan.
authors.forename: Nobuaki
authors.initials: N
authors.lastname: Matsumori
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Umegawa
authors.forename: Tohru
authors.initials: T
authors.lastname: Oishi
authors.forename: Michio
authors.initials: M
authors.lastname: Murata
mesh_terms: D000666:Amphotericin B / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D005461:Fluorine / Q000737:chemistry*; D006801:Humans; D007473:Ion Channels / Q000378:metabolism; D018942:Macrolides / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D013237:Stereoisomerism
chemical_list: D000935:Antifungal Agents; D007473:Ion Channels; D018942:Macrolides; D005461:Fluorine; D000666:Amphotericin B