title: Synthesis and biological evaluation of 1beta-methylcarbapenems having guanidino moieties.
abstract: The synthesis of a new series of 1beta-methylcarbapenems having the substituted guanidinocarbonyl pyrrolidine moieties is described. Their in vitro antibacterial activities against both Gram-positive including MRSA and Gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. In particular, the compound Ib having piperazinylguanidine moiety showed the most potent antibacterial activity.
authors.affiliation: Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul 130-650, South Korea. choh@kist.re.kr
authors.forename: Chang-Hyun
authors.initials: CH
authors.lastname: Oh
authors.forename: Jung-Hyuck
authors.initials: JH
authors.lastname: Cho
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015780:Carbapenems / Q000138:chemical synthesis* / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006146:Guanidines / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D011759:Pyrrolidines / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: C476323:1 beta-methylcarbapenem; D000900:Anti-Bacterial Agents; D015780:Carbapenems; D006146:Guanidines; D011759:Pyrrolidines