脂肽类抗真菌抗生素中的化学多样性。

Chemical diversity in lipopeptide antifungal antibiotics.

作者信息

Hino M, Fujie A, Iwamoto T, Hori Y, Hashimoto M, Tsurumi Y, Sakamoto K, Takase S, Hashimoto S

机构信息

Exploratory Research Laboratories, Fujisawa Pharmaceutical Co, Ltd, Tsukuba, Ibaraki, Japan.

出版信息

J Ind Microbiol Biotechnol. 2001 Sep;27(3):157-62. doi: 10.1038/sj.jim.7000091.

DOI:10.1038/sj.jim.7000091

PMID:11780786

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.

摘要

在筛选抗真菌抗生素的过程中，我们发现了一系列新型脂肽化合物，它们在结构上与棘白菌素B相关，但由于存在硫酸根残基，其水溶性比棘白菌素B高得多。这些化合物，即WF11899s、WF738s、WF14573s、WF16616和WF22210，及其衍生物在核结构和酰基侧链方面具有多样性。产生菌株分为两组，即腔孢纲真菌组和丝孢纲真菌组。WF11899A的衍生物化合物FK463目前正作为一种新型抗真菌抗生素处于3期临床开发阶段。