title: Synthesis and antibacterial activity of new carbapenems containing isoxazole moiety.
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.
authors.affiliation: Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul, South Korea.
authors.forename: Y K
authors.initials: YK
authors.lastname: Kang
authors.forename: K J
authors.initials: KJ
authors.lastname: Shin
authors.forename: K H
authors.initials: KH
authors.lastname: Yoo
authors.forename: K J
authors.initials: KJ
authors.lastname: Seo
authors.forename: C Y
authors.initials: CY
authors.lastname: Hong
authors.forename: C S
authors.initials: CS
authors.lastname: Lee
authors.forename: S Y
authors.initials: SY
authors.lastname: Park
authors.forename: D J
authors.initials: DJ
authors.lastname: Kim
authors.forename: S W
authors.initials: SW
authors.lastname: Park
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015780:Carbapenems / Q000138:chemical synthesis / Q000494:pharmacology; D004150:Dipeptidases / Q000378:metabolism; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013237:Stereoisomerism
chemical_list: D000900:Anti-Bacterial Agents; D015780:Carbapenems; D007555:Isoxazoles; D004150:Dipeptidases; C038937:dipeptidase