title: The synthesis and anti-MRSA activity of amidinium-substituted 2-dibenzofuranylcarbapenems.
abstract: A series of amidinium-substituted 2-dibenzofuranylcarbapenems with potent activity against MRSA has been synthesized via a Stille cross-coupling reaction. These new carbapenems show reduced serum protein binding and improved in vivo efficacy as a consequence of the positively charged amidinium substituent.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, NJ 07065, USA.
authors.forename: J B
authors.initials: JB
authors.lastname: Laub
authors.forename: M L
authors.initials: ML
authors.lastname: Greenlee
authors.forename: F
authors.initials: F
authors.lastname: DiNinno
authors.forename: J L
authors.initials: JL
authors.lastname: Huber
authors.forename: J G
authors.initials: JG
authors.lastname: Sundelof
mesh_terms: D000578:Amidines / Q000737:chemistry*; D015780:Carbapenems / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects*
chemical_list: D000578:Amidines; D015780:Carbapenems