Synthesis and biological activity of 1beta-methyl-2-[5-(2-N-substituted aminoethylcarbamoyl)pyrrolidin-3-ylthio]carbapenem derivatives.
The synthesis of a new series of 1beta-methylcarbapenems having the substituted aminoethylcarbamoylpyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive including MRSA and Gram-negative bacteria were tested and the effect of substituent on the pyrrolidine ring was investigated. In particular, the compound 11g having piperazinyl urea moiety showed the most potent antibacterial activity and 11k exhibited excellent anti-MRSA.
Oh
Chang-Hyun
CH
Medicinal Chemistry Research Center, Korea Institute of Science and Technology, 130-650, Seoul, South Korea.
Lee
Su-Chul
SC
Cho
Jung-Hyuck
JH
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D015780:Carbapenems / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D011759:Pyrrolidines / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D015780:Carbapenems; D011759:Pyrrolidines; C032519:pyrrolidine