title: Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 2: J-111,225, J-114,870, J-114,871 and related compounds.
abstract: Through further derivatization of J-111,347 (1a), a trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenem, undesired epileptogenicity in a rat intracerebroventricular assay (200 microg/rat) could be eliminated to afford J-111,225 (2a), J-114,870 (3a) and J-114,871 (3b) which preserved comparable broad antimicrobial activity.
authors.affiliation: Banyu Tsukuba Research Institute, Ibaraki, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Imamura
authors.forename: N
authors.initials: N
authors.lastname: Ohtake
authors.forename: A
authors.initials: A
authors.lastname: Shimizu
authors.forename: H
authors.initials: H
authors.lastname: Sato
authors.forename: Y
authors.initials: Y
authors.lastname: Sugimoto
authors.forename: S
authors.initials: S
authors.lastname: Sakuraba
authors.forename: H
authors.initials: H
authors.lastname: Kiyonaga
authors.forename: C
authors.initials: C
authors.lastname: Suzuki-Sato
authors.forename: M
authors.initials: M
authors.lastname: Nakano
authors.forename: R
authors.initials: R
authors.lastname: Nagano
authors.forename: K
authors.initials: K
authors.lastname: Yamada
authors.forename: T
authors.initials: T
authors.lastname: Hashizume
authors.forename: H
authors.initials: H
authors.lastname: Morishima
mesh_terms: D015780:Carbapenems / Q000138:chemical synthesis* / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D013210:Staphylococcus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D015780:Carbapenems; C404721:J 111225; C404722:J 114870; D011759:Pyrrolidines