STUDIES ON THE SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF 2-(2-FUNCTIONALIZED PYRROLIDIN-4-YLTHIO)-1-BETA-METHYLCARBAPENEMS

A series of new carbapenem derivatives, which have a pyrrolidin-4-ylth io group substituted with a hydroxyalkyl or carbamoyl group at the 2' position as the C-2 side chain, have been prepared. The antibacterial activity and the stability to renal dehydropeptidase-I of these compou nds were investigated, and the structure-activity relationships were s tudied. Among these new carbapenems, ydroxyethyl]-1-methyl-1-carbapen- 2-em-3-carboxylic acid (la) showed the most potent and well balanced a ctivity and was selected as a candidate for further evaluation.