新型索德菌素衍生物FR290581：合成与抗真菌活性
FR290581, a novel sordarin derivative: synthesis and antifungal activity.
作者信息
Hanadate Tadaatsu, Tomishima Masaki, Shiraishi Nobuyuki, Tanabe Daisuke, Morikawa Hiroshi, Barrett David, Matsumoto Satoru, Ohtomo Kazumi, Maki Katsuyuki
机构信息
Chemistry Research Labs., Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan.
出版信息
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1465-8. doi: 10.1016/j.bmcl.2009.01.051. Epub 2009 Jan 22.
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.
索德菌素是一种独特的天然产物抗真菌剂，它是延伸因子2的抑制剂。为了提高生物活性，我们通过对苷元索德菌素进行新型修饰合成了各种化合物。结果，我们发现了新型索德菌素衍生物FR290581。该化合物表现出优异的活性和良好的药代动力学特征，并且对白色念珠菌也显示出良好的体内活性。
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