Abstract
Armeniaspiroles, a novel class of natural products isolated from Streptomyces armeniacus, are characterized by a novel spiro[4.4]non-8-ene scaffold. Various derivatives of Armeniaspiroles could be obtained by halogenation, alkylation, addition/elimination or reductions. A total synthesis of the 5-chloro analog of Armeniaspirole A has been accomplished in a linear six-step sequence. 5-Chloro-Armeniaspirole A exhibits good activity against a range of multidrug-resistant, Gram-positive bacterial pathogens.
Copyright © 2012 Elsevier Ltd. All rights reserved.
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 / isolation & purification
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Anti-Bacterial Agents / pharmacology*
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Biological Products / chemical synthesis
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Biological Products / chemistry
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Biological Products / isolation & purification
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Biological Products / pharmacology
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Dose-Response Relationship, Drug
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Drug Resistance, Multiple, Bacterial / drug effects*
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ERG1 Potassium Channel
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Enterococcus faecium / drug effects
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Enterococcus faecium / growth & development
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Ether-A-Go-Go Potassium Channels / antagonists & inhibitors
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Humans
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Lactams / chemistry
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Lactams / isolation & purification
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Lactams / pharmacology*
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Male
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Methicillin-Resistant Staphylococcus aureus / drug effects
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Methicillin-Resistant Staphylococcus aureus / growth & development
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Mice
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Molecular Structure
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Spiro Compounds / chemistry
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Spiro Compounds / isolation & purification
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Spiro Compounds / pharmacology*
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Streptococcus pneumoniae / drug effects
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Streptococcus pneumoniae / growth & development
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Structure-Activity Relationship
Substances
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5-chloro-armeniaspirole A
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Anti-Bacterial Agents
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Biological Products
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels
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Lactams
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Spiro Compounds