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Bioorg Med Chem Lett ; 19(5): 1465-8, 2009 Mar 01.
Article in English | MEDLINE | ID: mdl-19196509

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.


Subject(s)
Antifungal Agents/chemical synthesis , Indenes/chemical synthesis , Animals , Antifungal Agents/pharmacology , Candida albicans/drug effects , Candida albicans/metabolism , Indenes/pharmacology , Mice , Protein Synthesis Inhibitors/chemical synthesis , Structure-Activity Relationship
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