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Antibiotics U 1200Synthesis and Antibacterial Activity of 1β-Methyl-2-[5-(1,2-disubstituted ethyl)pyrrolidin-3-ylthio]carbapenem Derivatives. Part 3. -A series of title compounds such as (IV) and (XI) is prepared according to the scheme and tested against both Gram-positive and Gram-negative bacteria. Among them, derivative (IVa) exhibits the most potent antibacterial activity. -(CHO, J.-H.; AHN, S.-H.; JEON, H.; KIM, S. Y.; OH*, C.-H.; Bull. Korean Chem.

Pyrazine derivatives R 0550 Solution-Phase Synthesis and Preliminary Evaluation of 1,6,8-Trisubstituted Tetrahydro-2H-pyrazino[1,2-a]pyrimidin-4,7-dione Derivatives as a NF-kBInhibitor. -Compounds (VIIIb) and (VIIIc) exhibit a 40% inhibition of the target NF-kB 549 [for compound (V) no yield given]. -(KIM, J.-W.; LEE, S.-C.; PARK, H. B.; JO, N. H.; YOO, K. H.; CHO, J.-H.; OH*, C.-H.; Bull. Korean Chem.

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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.