Abstract
The echinocandin class of cyclic lipopeptides has been simplified to discover potent antifungal compounds. Namely A-192411 shows good in vitro activity against common pathogenic yeasts and has an acceptable safety window in vivo. Discovery, limited SAR, synthesis, biochemical and pharmaco-dynamic profiles of A-192411 are presented.
MeSH terms
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Animals
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Antifungal Agents / chemical synthesis*
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Antifungal Agents / pharmacokinetics
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Antifungal Agents / pharmacology*
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Area Under Curve
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Candida / drug effects
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Candida / metabolism
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Candidiasis / drug therapy
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Candidiasis / microbiology
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Chemical Phenomena
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Chemistry, Physical
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Dogs
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Drug Design
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Fungi / drug effects
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Fungi / metabolism*
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Glucans / metabolism
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Haplorhini
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Mice
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Microbial Sensitivity Tests
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Oligopeptides / chemical synthesis*
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Oligopeptides / pharmacokinetics
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Oligopeptides / pharmacology*
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RNA, Fungal / biosynthesis
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Rats
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Structure-Activity Relationship
Substances
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A-192411
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Antifungal Agents
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Glucans
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Oligopeptides
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RNA, Fungal