FR290581, a novel sordarin derivative: Synthesis and antifungal activity |
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| Authors: | Tadaatsu Hanadate Masaki Tomishima Nobuyuki Shiraishi Daisuke Tanabe Hiroshi Morikawa David Barrett Satoru Matsumoto Kazumi Ohtomo Katsuyuki Maki |
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| Affiliation: | 1. Chemistry Research Labs., Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan;2. Pharmacology Research Labs., Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan |
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| Abstract: | Sordarin is a unique natural product antifungal agent that is an inhibitor of elongation factor 2. To improve biological activity, we synthesized various compounds by novel modification of the aglycone, sordaricin. As a result, we have discovered the novel sordarin derivative FR290581. This compound exhibited superior activity and a good pharmacokinetic profile, and also displayed good in vivo activity against Candida albicans. |
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