Novel 1β-methylcarbapenems with isoxazoloethenyl moieties containing carboxylic acid sodium salt
The synthesis of novel 1β-methylcarbapenems 1a,b having sodium 5-(3- and 5-carboxylic acid)isoxazoloethenyl moieties at C-5 position of pyrrolidine ring and their biological evaluation are described. Both compounds showed potent and well-balanced antibacterial activity as well as high stability to DHP-I. The selected sodium 3-carboxylic acid derivative 1a possessed excellent DHP-I stability and advanced pharmacokinetic parameters in comparison with 2 and meropenem. The synthesis of novel 1β-methylcarbapenems 1a,b having sodium 5-(3- and 5-carboxylic acid)isoxazoloethenyl moieties at C-5 position of pyrrolidine ring and their biological evaluation are described. Both compounds showed potent and well-balanced antibacterial activity as well as high stability to DHP-I. The selected sodium 3-carboxylic acid derivative 1a possessed excellent DHP-I stability and advanced pharmacokinetic parameters in comparison with 2 and meropenem.
1?-METHYLCARBAPENEM DERIVATIVE AND PROCESS FOR THE PREPARATION THEREOF
The present invention relates to a novel 1β-methylcarbapenem derivative, a process for the preparation thereof and a pharmaceutical composition comprising the 1β-methylcarbapenem derivative or a pharmaceutically acceptable salt thereof as an active antiba
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(2010/02/15)
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