化学
抗真菌
棘白菌素
体内
全合成
化学合成
残留物(化学)
立体化学
结构-活动关系
白霉素类
体外
药理学
组合化学
生物化学
两性霉素B
微生物学
氟康唑
生物技术
卡斯波芬金
医学
生物
作者
Larry L. Klein,Leping Li,Hui-Ju Chen,Cynthia B. Curty,David A. DeGoey,David J. Grampovnik,Christina L. Leone,Samuel Thomas,Clinton M. Yeung,Kenneth W. Funk,Vimal Kishore,Edwin O. Lundell,Dariusz Wódka,Jonathan A. Meulbroek,Jeffrey Alder,Angela M. Nilius,Paul A. Lartey,Jacob J. Plattner
标识
DOI:10.1016/s0968-0896(00)00097-3
摘要
The need for new therapies to treat systemic fungal infections continues to rise. Naturally occurring hexapeptide echinocandin B (1) has shown potent antifungal activity via its inhibition of the synthesis of beta-1,3 glucan, a key fungal cell wall component. Although this series of agents has been limited thus far based on their physicochemical characteristics, we have found that the synthesis of analogues bearing an aminoproline residue in the 'northwest' position imparts greatly improved water solubility (> 5 mg/mL). The synthesis and structure-activity relationships (SAR) based on whole cell and upon in vivo activity of the series of compounds are reported.
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