Abstract
A series of novel pleuromutilin derivatives possessing thioether moiety has been synthesized via acylation reaction under mild conditions. Their in vitro antibacterial activity against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae were tested by agar dilution method and Oxford cup assay. Among the 17 compounds screened, 14-O-[(4-methoxybenzamide-2- methylpropane-2-yl) thioacetate] mutilin 4i, 14-O-[(2-aminobenzamide-2-methylpropane-2-yl) thioacetate] mutilin 5a and 14-O-[(4-aminobenzamide-2-methylpropane-2-yl) thioacetate] mutilin 5c were resulted as most active antibacterial agents.
Crown Copyright © 2013. Published by Elsevier Masson SAS. All rights reserved.
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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Benzamides / chemical synthesis
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Benzamides / chemistry
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Benzamides / pharmacology
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Diterpenes / chemical synthesis
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Diterpenes / chemistry
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Diterpenes / pharmacology
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Escherichia coli / drug effects
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Methicillin Resistance / drug effects
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Methicillin-Resistant Staphylococcus aureus / drug effects
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Microbial Sensitivity Tests
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Models, Chemical
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Molecular Structure
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Pleuromutilins
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Polycyclic Compounds / chemical synthesis
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Polycyclic Compounds / chemistry
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Polycyclic Compounds / pharmacology
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Staphylococcus epidermidis / drug effects
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Streptococcus agalactiae / drug effects
Substances
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14-O-((4-aminobenzamide-2-methylpropane-2-yl)thioacetate)mutilin
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Anti-Bacterial Agents
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Benzamides
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Diterpenes
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Polycyclic Compounds