Abstract
A series of C-12 pyrazolinyl spiro ketolide derivatives were designed and synthesized. The C-12 modifications involved replacing the natural C-12 methyl group in clarithromycin core with different pyrazolinyl spiros via chemical synthesis. Potential anti-bacterial activities against both erythromycin-susceptible and erythromycin-resistant bacteria were reported.
Copyright © 2010 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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Drug Resistance, Bacterial / drug effects*
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Haemophilus influenzae / drug effects
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Ketolides / chemical synthesis
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Ketolides / chemistry
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Ketolides / pharmacology*
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Microbial Sensitivity Tests
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Molecular Conformation
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Pyrazoles / chemical synthesis
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Pyrazoles / chemistry
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Pyrazoles / pharmacology*
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Spiro Compounds / chemical synthesis
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Spiro Compounds / chemistry
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Spiro Compounds / pharmacology*
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Staphylococcus / drug effects
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Ketolides
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Pyrazoles
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Spiro Compounds