title: Novel 1beta-methylcarbapenems with isoxazoloethenyl moieties containing carboxylic acid sodium salt.
abstract: The synthesis of novel 1beta-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.
authors.affiliation: Medicinal Chemistry Research Center, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Korea.
authors.forename: Kyung Seok
authors.initials: KS
authors.lastname: Lee
authors.forename: Yong Koo
authors.initials: YK
authors.lastname: Kang
authors.forename: Kyung Ho
authors.initials: KH
authors.lastname: Yoo
authors.forename: Dong Chan
authors.initials: DC
authors.lastname: Kim
authors.forename: Kye Jung
authors.initials: KJ
authors.lastname: Shin
authors.forename: Young-Sook
authors.initials: YS
authors.lastname: Paik
authors.forename: Dong Jin
authors.initials: DJ
authors.lastname: Kim
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D019540:Area Under Curve; D015780:Carbapenems / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000032:analysis*; D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D008826:Microbial Sensitivity Tests
chemical_list: C476323:1 beta-methylcarbapenem; D000900:Anti-Bacterial Agents; D015780:Carbapenems; D002264:Carboxylic Acids