FR290581, a novel sordarin derivative: synthesis and antifungal activity.

Bioorg Med Chem Lett

Chemistry Research Labs., Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan.

Published: March 2009

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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http://dx.doi.org/10.1016/j.bmcl.2009.01.051DOI Listing

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