title: Synthesis and biological activity of 1beta-methyl-2-[5'-isoxazoloethenylpyrrolidin-3'-ylthio]carbapenems.
abstract: A new series of 1beta-methylcarbapenems 1a-i bearing isoxazoloethenyl groups on the pyrrolidine ring has been prepared and evaluated for in vitro antibacterial activity and stability to DHP-I. Most compounds showed excellent antibacterial activity and high stability to DHP-I superior to that of meropenem. Of these new carbapenems, 1a,b,h exhibited the best combination of antibacterial activity and DHP-I stability.
authors.affiliation: Life Sciences Division, Korea Institute of Science and Technology, Cheongryang, Seoul, South Korea. djk2991@kist.re.kr
authors.forename: D J
authors.initials: DJ
authors.lastname: Kim
authors.forename: K J
authors.initials: KJ
authors.lastname: Seo
authors.forename: K S
authors.initials: KS
authors.lastname: Lee
authors.forename: K J
authors.initials: KJ
authors.lastname: Shin
authors.forename: K H
authors.initials: KH
authors.lastname: Yoo
authors.forename: D C
authors.initials: DC
authors.lastname: Kim
authors.forename: S W
authors.initials: SW
authors.lastname: Park
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D015780:Carbapenems / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D004150:Dipeptidases / Q000378:metabolism; D004355:Drug Stability; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007555:Isoxazoles / Q000494:pharmacology*; D000077731:Meropenem; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D013552:Swine; D013845:Thienamycins / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D015780:Carbapenems; D007555:Isoxazoles; D013845:Thienamycins; D004150:Dipeptidases; C038937:dipeptidase; D000077731:Meropenem