Synthesis and antibacterial activity of 1 beta-methyl-2-(5-substituted imidazolino pyrrolidin-3-ylthio)carbapenem derivatives.
The synthesis of a new series of 1 beta-methylcarbapenems containing a substituted imidazolino pyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of the substituent on the imidazoline ring was investigated. Compound 13 g which has a N-sulfonylmethyl substituted imidazoline moiety showed the most potent antibacterial activity.
Oh
Chang-Hyun
CH
Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul 130-650, Korea. choh@kist.re.kr
Lee
Chang-Sik
CS
Lee
Jong-Sun
JS
Cho
Jung-Hyuck
JH
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015780:Carbapenems / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004355:Drug Stability; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D015780:Carbapenems; D011759:Pyrrolidines