Abstract
The synthesis and biological properties of a novel water-soluble echinocandin-like lipopeptide, FR131535, are described. This compound displayed potent in vitro and in vivo antifungal activities. The hemolytic activity of FR901379 was reduced by replacing the acyl side chain. This compound showed good water-solubility, comparable to the natural product FR901379.
MeSH terms
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Animals
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology
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Antifungal Agents / chemical synthesis*
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Antifungal Agents / pharmacology
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Antifungal Agents / toxicity
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Bronchogenic Cyst / drug therapy
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Candida albicans / drug effects
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Candida albicans / enzymology
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Candidiasis / drug therapy
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Disease Models, Animal
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Echinocandins
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Female
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Fungal Proteins*
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Glucosyltransferases / antagonists & inhibitors*
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Hemolysis / drug effects
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Membrane Proteins*
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Mice
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Mice, Nude
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Peptides*
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Peptides, Cyclic / chemical synthesis
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Peptides, Cyclic / pharmacology*
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Peptides, Cyclic / toxicity
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Pneumonia, Pneumocystis / drug therapy
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Schizosaccharomyces pombe Proteins*
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Solubility
Substances
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Anti-Bacterial Agents
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Antifungal Agents
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Echinocandins
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FR 131535
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Fungal Proteins
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Membrane Proteins
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Peptides
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Peptides, Cyclic
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Schizosaccharomyces pombe Proteins
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echinocandin B
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Glucosyltransferases
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1,3-beta-glucan synthase