title: Structure-activity relationships of trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems. Part 1: J-111,347 and related compounds.
abstract: 1Beta-methylcarbapenems having various 3,5-disubstituted pyrrolidinylthio-side chains at C-2 were designed and synthesized. Evaluation of their antibacterial activities indicated that J-111,347 (1a) is the first example of an extremely broad spectrum antibiotic showing activity against methicillin-resistant Staphylococcus aureus (MRSA) as well as Pseudomonas aeruginosa.
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: Jona
authors.forename: H
authors.initials: H
authors.lastname: Sato
authors.forename: R
authors.initials: R
authors.lastname: Nagano
authors.forename: R
authors.initials: R
authors.lastname: Ushijima
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: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015780:Carbapenems / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D015394:Molecular Structure; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D015780:Carbapenems; C404720:J 111347; D011759:Pyrrolidines