1 beta-Methyl-2-(5-substituted pyrrolidin-3-ylthio)carbapenems. 2. Synthesis and antibacterial activity of 5-aminopropyl and 5-aminopropenyl pyrrolidine derivatives.
The synthesis and biological activity of (1 R, 5S, 6S)-2-[(3S, 5S)-5-substituted pyrrolidin-3-ylthio]-6-[(R)-1-hydroxyethyl]-1-methyl-1- carbapen-2-em-3-carboxylic acid, in which aminopropyl, aminopropenyl, and aminopropynyl groups were introduced as substituents, are described. Aminopropyl and aminopropenyl derivatives showed potent in vitro and in vivo antibacterial activity against Gram-positive and Gram-negative bacteria including P. aeruginosa.
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd., Japan.
N
N
Ohtake
O
O
Okamoto
S
S
Kato
R
R
Ushijima
H
H
Fukatsu
S
S
Nakagawa
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D015780:Carbapenems / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D013055:Spectrophotometry, Infrared
D000900:Anti-Bacterial Agents; D015780:Carbapenems