Novel echinocandin antifungals. Part 1: novel side-chain analogs of the natural product FR901379 |
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| Authors: | Tomishima Masaki Ohki Hidenori Yamada Akira Maki Katsuyuki Ikeda Fumiaki |
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| Affiliation: | Medicinal Chemistry Research Laboratories, Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan. |
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| Abstract: | 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. |
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