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The synthesis of a new series of 1beta-methylcarbapenems having spiro[2,4]heptane moieties is described. Their in-vitro antibacterial activities against both gram-positive and gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. Most compounds were shown to be more active than the compared meropenem and imipenem against Escherichia coli. One particular compound, IIIb, having hydroxy a moiety showed the most potent antibacterial activity.

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Activity. -The general route to the new carbapenems involves the preparation of appropriately protected thiols containing a pyrrolidine ring as a side chain [cf. (IV)] and coupling with the carbapenem diphenylphosphate (V), followed by deprotection of the carbapenems (VI) in the usual fashion. Comparative in vitro studies of selected carbapenem, meropenem, and imipenem against 40 bacterial strains show that deprotected (VIc) possesses excellent activity against the target pathogens, except P. aeruginosa, and similar or superior antibacterial activities against Gram-positive bacteria compared to meropenem, as well as against Gram-negative bacteria compared to imipenem. -(KIM, S. J.; PARK, H. B.; LEE, J. S.; JO, N. H.; YOO, K. H.; BAEK, D.; KANG, B.-W.; CHO, J.-H.; OH*, C.-H.; Eur.