Novel echinocandin antifungals. Part 1: Novel side-chain analogs of the natural product FR901379

descriptionPublicationkeyboard_double_arrow_right Article 01 Feb 2008 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 18, pages 1,474-1,477 (issn: 0960-894X,

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Authors: Masaki, Tomishima; Hidenori, Ohki; Akira, Yamada; Katsuyuki, Maki; Fumiaki, Ikeda;

doi: 10.1016/j.bmcl.2007.12.062

pmid: 18207736

Novel echinocandin antifungals. Part 1: Novel side-chain analogs of the natural product FR901379

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Abstract

A series of novel acylated analogs of the novel water-soluble echinocandin FR901379 have been prepared and evaluated for antifungal and hemolytic activity. A relationship between antifungal activity and lipophilicity of the acyl side chain, expressed as ClogP was demonstrated, and an analog (3c) with 5.5- to 8-fold superior in vivo activity relative to the previously disclosed 4-(n-octyloxy)benzoyl side chain analog, FR131535 obtained.

Related Organizations

Astellas Pharma (Japan)
Japan

Keywords

Echinocandins, Structure-Activity Relationship, Antifungal Agents, Hemolytic Agents, Aspergillus fumigatus, Candida albicans, Peptides, Cyclic

8 Research products, page 1 of 1

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