Abstract
The synthesis and biological activity of a series of new 1beta-methylcarbapenems 1a-g containing 5'-isoxazolopyrrolidin-3'-ylthio derivatives as C-2 side chain are described. Most compounds exhibited potent and well-balanced antibacterial activity as well as high stability to DHP-I comparable to that of meropenem. 1e and 1c showed the best combination of antibacterial activity and stability to DHP-I, respectively.
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 / pharmacology
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Carbapenems / chemical synthesis
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Carbapenems / pharmacology
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Dipeptidases / metabolism
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Gram-Negative Bacteria / drug effects
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Gram-Positive Bacteria / drug effects
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Isoxazoles / chemical synthesis*
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Isoxazoles / pharmacology
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Microbial Sensitivity Tests
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Molecular Structure
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Stereoisomerism
Substances
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Anti-Bacterial Agents
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Carbapenems
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Isoxazoles
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Dipeptidases
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dipeptidase