Abstract
The synthesis and biological activity of a series of N-alkylated derivatives of echinocandin B are described and compared with the N-acylated analogs. The linear, rigid geometry of the side chain that was essential to improve the antifungal potency of the N-acylated series gave similar in vitro results with the N-alkylated derivatives. However the slight structural variation forfeited all in vivo activity.
MeSH terms
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Animals
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Anti-Bacterial Agents / chemical synthesis
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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 / chemistry*
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Antifungal Agents / pharmacology*
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Candidiasis / drug therapy*
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Chromatography, High Pressure Liquid
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Echinocandins
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Fungal Proteins*
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Humans
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Mass Spectrometry
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Mice
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Microbial Sensitivity Tests
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Peptides*
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Peptides, Cyclic*
Substances
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Anti-Bacterial Agents
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Antifungal Agents
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Echinocandins
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Fungal Proteins
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Peptides
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Peptides, Cyclic
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echinocandin B