title: Dicationic 2-fluorenonylcarbapenems: potent anti-MRS agents with improved solubility and pharmacokinetic properties.
abstract: The synthesis and biological evaluation of a series of dicationic-substituted 2-fluorenonylcarbapenems is described. This class of compounds showed enhanced water solubility while maintaining potent activity against MRS. Introduction of a 1-beta-methyl substituent was found to improve pharmacokinetics.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
authors.forename: M L
authors.initials: ML
authors.lastname: Greenlee
authors.forename: J B
authors.initials: JB
authors.lastname: Laub
authors.forename: G P
authors.initials: GP
authors.lastname: Rouen
authors.forename: F
authors.initials: F
authors.lastname: DiNinno
authors.forename: M L
authors.initials: ML
authors.lastname: Hammond
authors.forename: J L
authors.initials: JL
authors.lastname: Huber
authors.forename: J G
authors.initials: JG
authors.lastname: Sundelof
authors.forename: G G
authors.initials: GG
authors.lastname: Hammond
mesh_terms: D000818:Animals; D015780:Carbapenems / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D002412:Cations; D006207:Half-Life; D008253:Macaca mulatta; D016106:Methicillin Resistance; D051379:Mice; D008826:Microbial Sensitivity Tests; D012995:Solubility; D013203:Staphylococcal Infections / Q000188:drug therapy; D013211:Staphylococcus aureus / Q000187:drug effects*
chemical_list: D015780:Carbapenems; D002412:Cations