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.
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.
Imamura
H
H
Banyu Tsukuba Research Institute, Ibaraki, Japan.
Ohtake
N
N
Shimizu
A
A
Sato
H
H
Sugimoto
Y
Y
Sakuraba
S
S
Kiyonaga
H
H
Suzuki-Sato
C
C
Nakano
M
M
Nagano
R
R
Yamada
K
K
Hashizume
T
T
Morishima
H
H
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
D015780:Carbapenems; C404721:J 111225; C404722:J 114870; D011759:Pyrrolidines