Tomishima Masaki, Ohki Hidenori, Yamada Akira, Maki Katsuyuki, Ikeda Fumiaki
Medicinal Chemistry Research Laboratories, Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan.
Bioorg Med Chem Lett. 2008 Feb 15;18(4):1474-7. doi: 10.1016/j.bmcl.2007.12.062. Epub 2007 Dec 28.
A series of novel acylated analogs of the novel water-soluble echinocandin FR901379 have been prepared and evaluated for antifungal and hemolytic activity. A relationship between antifungal activity and lipophilicity of the acyl side chain, expressed as ClogP was demonstrated, and an analog (3c) with 5.5- to 8-fold superior in vivo activity relative to the previously disclosed 4-(n-octyloxy)benzoyl side chain analog, FR131535 obtained.
已经制备了一系列新型水溶性棘白菌素FR901379的酰化类似物，并对其抗真菌和溶血活性进行了评估。结果表明，抗真菌活性与以ClogP表示的酰基侧链亲脂性之间存在关联，并且获得了一种体内活性比先前公开的具有4-(正辛氧基)苯甲酰基侧链的类似物FR131535高5.5至8倍的类似物(3c)。
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