Synthesis and biological evaluation of 1β-methylcarbapenems having guanidino moieties

The synthesis of a new series of 1β-methylcarbapenems having the substituted guanidinocarbonyl pyrrolidine moieties is described. Their in vitro antibacterial activities against both Gram-positive including MRSA and Gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. In particular, the compound Ib having piperazinylguanidine moiety showed the most potent antibacterial activity.

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