Synthesis and biological activity of novel macrocyclic antifungals. modification of the tyrosine moiety of the lipopeptidolactone FR901469.

Abstract	A series of tyrosine-modified derivatives of the macrocyclic lipopeptidolactone FR901469 have been prepared and evaluated for in vitro and in vivo antifungal activity and for hemolytic activity towards red blood cells. Compound 14 displayed significantly reduced hemolytic potential at 1mg/mL and a comparable protective effect to FR901469 in a mouse candidiasis model.
Authors	D Barrett, A Tanaka, K Harada, E Watabe, K Maki, F Ikeda
Journal	Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 11 Issue 14 Pg. 1843-9 (Jul 23 2001) ISSN: 0960-894X [Print] England
PMID	11459644 (Publication Type: Journal Article)
Chemical References	Antifungal Agents Depsipeptides FR 901469 Lactones Peptides, Cyclic Tyrosine
Topics	Animals Antifungal Agents (chemical synthesis, pharmacology) Candida albicans (cytology, pathogenicity) Candidiasis (drug therapy, microbiology) Depsipeptides Erythrocytes (drug effects) Hemolysis (drug effects) Lactones (chemical synthesis, pharmacology) Mice Microbial Sensitivity Tests (standards) Peptides, Cyclic (chemical synthesis, chemistry, pharmacology) Tyrosine (analogs & derivatives, chemistry)

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