ChemInform Abstract: Novel 1β‐Methylcarbapenems Having Cyclic Sulfonamide Moieties: Synthesis and Evaluation of in vitro Antibacterial Activity.

Abstract

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.