title: Synthesis and biological evaluation of novel 1beta-methylcarbapenems having a new moiety at C-2.
abstract: The synthesis and biological activity of the novel series of 1 beta-methylcarbapenems 1a-f, bearing a variety of 3",4"-disubstituted pyrrolidinamides as substituents at C-2, are described. Of these carbapenems, diol 1a showed the most potent and well balanced antibacterial activity against Gram-positive and Gram-negative. 1a was also evaluated for pharmacokinetics and in vivo therapeutic efficacy in systemic infections.
authors.affiliation: Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul.
authors.forename: Y K
authors.initials: YK
authors.lastname: Kang
authors.forename: K J
authors.initials: KJ
authors.lastname: Shin
authors.forename: K H
authors.initials: KH
authors.lastname: Yoo
authors.forename: K J
authors.initials: KJ
authors.lastname: Seo
authors.forename: S Y
authors.initials: SY
authors.lastname: Park
authors.forename: D J
authors.initials: DJ
authors.lastname: Kim
authors.forename: S W
authors.initials: SW
authors.lastname: Park
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D001682:Biological Availability; D015780:Carbapenems / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D051379:Mice; D008826:Microbial Sensitivity Tests
chemical_list: D000900:Anti-Bacterial Agents; D015780:Carbapenems