FR290581, a novel sordarin derivative: Synthesis and antifungal activity

We have discovered the novel sordarin derivative FR290581, which exhibited superior activity, a good pharmacokinetic profile and good in vivo activity. 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.