Abstract
In the course of our research aimed at the discovery of metabolic stable pleuromutilin derivatives with more potent antibacterial activity against Gram-positive pathogens than previous analogues, a series of compounds bearing a purine ring were prepared and evaluated. From SAR studies, we identified two promising compounds 85 and 87, which have excellent in vitro activity against a number of Gram-positive pathogens, including existing drug-resistant strains, and potent in vivo efficacy.
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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Diterpenes / chemical synthesis
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Diterpenes / chemistry
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Diterpenes / pharmacology*
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Dose-Response Relationship, Drug
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Drug Resistance, Bacterial
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Gram-Positive Bacteria / drug effects*
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Gram-Positive Bacteria / growth & development
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Microbial Sensitivity Tests
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Molecular Structure
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Pleuromutilins
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Polycyclic Compounds
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Purines / chemical synthesis
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Purines / chemistry
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Purines / pharmacology*
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Solubility
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Diterpenes
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Polycyclic Compounds
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Purines
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purine