Synthesis and antibacterial activity of 1beta-methyl-2-[5-(N-substituted-2-hydroxy iminoethyl)pyrrolidin-3-ylthio]carbapenem derivatives.
The synthesis of a new series of 1-methylcarbapenems having the substituted thiazolopyrrolidine moiety is described. Their in vitro antibacterial activities against both gram-positive and gram-negative bacteria were tested and the effect of substituent on the pyrrolidine ring was investigated. In particular, compounds 12b and 12k showed the most potent antibacterial activity.
Oh
Chang-Hyun
CH
Medicinal Chemistry Research Center, Korea Institute of Science and Technology, P.O. Box 131, Cheongryang, 130-650, Seoul, South Korea.
Lee
Su-Chul
SC
Cho
Jung-Hyuck
JH
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D015780:Carbapenems / Q000138:chemical synthesis* / Q000494:pharmacology*; D004355:Drug Stability; D006090:Gram-Negative Bacteria / Q000187:drug effects / Q000254:growth & development; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000254:growth & development; D008826:Microbial Sensitivity Tests; D011550:Pseudomonas aeruginosa / Q000187:drug effects / Q000254:growth & development; D011759:Pyrrolidines / Q000737:chemistry; D013329:Structure-Activity Relationship; D013552:Swine
D000900:Anti-Bacterial Agents; D015780:Carbapenems; D011759:Pyrrolidines