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Chemical diversity in lipopeptide antifungal antibiotics
Authors:M Hino  A Fujie  T Iwamoto  Y Hori  M Hashimoto  Y Tsurumi  K Sakamoto  S Takase  S Hashimoto
Affiliation:Exploratory Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, Tsukuba, Ibaraki, Japan.
Abstract:In the course of screening for antifungal antibiotics, we have discovered a novel series of lipopeptide compounds structurally related to, but highly superior to, echinocandin B in terms of their water solubility due to the presence of a sulfate residue. These compounds, WF11899s, WF738s, WF14573s, WF16616 and WF22210, and their derivatives have diversity in their nuclear structures and acyl side chains. The producing strains were classified into two groups, the Coleomycetes group and the Hyphomycetes group. Compound FK463, a derivative of WF11899A, is currently in Phase 3 clinical development as a novel antifungal antibiotic.
Keywords:: antifungal compounds   lipopeptide   sulfate   Coleomycetes
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