1β-Methyl-2-(5-substituted pyrrolidin-3-ylthio)carbapenems; 2. Synthesis and Antibacterial Activity of 5-Aminopropyl and 5-Aminopropenyl Pyrrolidine Derivatives

Abstract

The synthesis and biological activity of (1R, 5S, 6S)-2-[(3S, 5S)-5-substituted pyrrolidin-3-ylthio]6-[(R)-1-hydroxyethyl]-1-methyl- l-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.