Abstract
We report the first total synthesis of micrococcin P2 (MP2, 1) by a diversity-oriented route that incorporates a number of refinements relative to earlier syntheses. Biological data regarding the activity of 1 against a range of human pathogens are also provided. Furthermore, we disclose a chemical property of MP2 that greatly facilitates medicinal chemistry work in the micrococcin area and describe a method to obtain MP2 by fermentation in B. subtilis.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Bacteriocins / chemistry
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Bacteriocins / pharmacology
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Microbial Sensitivity Tests
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Molecular Structure
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Mycobacterium tuberculosis* / drug effects
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Peptides, Cyclic* / chemical synthesis
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Peptides, Cyclic* / chemistry
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Peptides, Cyclic* / pharmacology
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Stereoisomerism
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Sulfhydryl Compounds* / chemical synthesis
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Sulfhydryl Compounds* / chemistry
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Sulfhydryl Compounds* / pharmacology
Substances
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Anti-Bacterial Agents
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Bacteriocins
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micrococcin
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Sulfhydryl Compounds
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micrococcin P2
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Peptides, Cyclic