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

Bioorganic & Medicinal Chemistry Letters
Masaki TomishimaFumiaki Ikeda

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.

References

Jun 27, 2002·Biochimica Et Biophysica Acta·David Barrett

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Citations

Jan 10, 2009·The Journal of Antibiotics·Seiji Hashimoto
Sep 30, 2008·Natural Product Reports·Kristina GrabowskiGisbert Schneider
Jul 15, 2011·Journal of Bioscience and Bioengineering·Satoshi UedaSeiji Hashimoto
Apr 24, 2013·Angewandte Chemie·Frauke Messik, Markus Oberthür
Oct 22, 2013·Natural Product Reports·Armin Bauer, Mark Brönstrup

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