title: Novel beta-lactam antibiotics synthesized by amination of catechols using fungal laccase.
abstract: Novel cephalosporins, penicillins, and carbacephems were synthesized by amination of catechols with amino-beta-lactams like cefadroxil, amoxicillin, ampicillin and the structurally related carbacephem loracarbef using laccase from Trametes sp. All isolated monoaminated products inhibited the growth of several Gram positive bacterial strains in the agar diffusion assay, among them methicillin-resistant Staphylococcus aureus strains and vancomycin-resistant Enterococci. Observed differences in the cytotoxicity and in vivo activity in a "Staphylococcus-infected, immune suppressed mouse" model are discussed.
authors.affiliation: Institute of Microbiology, Ernst-Moritz-Arndt-University Greifswald, Greifswald, Germany. annett.mikolasch@gmx.de
authors.forename: Annett
authors.initials: A
authors.lastname: Mikolasch
authors.forename: Martina
authors.initials: M
authors.lastname: Wurster
authors.forename: Michael
authors.initials: M
authors.lastname: Lalk
authors.forename: Sabine
authors.initials: S
authors.lastname: Witt
authors.forename: Simone
authors.initials: S
authors.lastname: Seefeldt
authors.forename: Elke
authors.initials: E
authors.lastname: Hammer
authors.forename: Frieder
authors.initials: F
authors.lastname: Schauer
authors.forename: Wolf-Dieter
authors.initials: WD
authors.lastname: Jülich
authors.forename: Ulrike
authors.initials: U
authors.lastname: Lindequist
mesh_terms: D000586:Amination; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002384:Catalysis; D002396:Catechols / Q000737:chemistry*; D005658:Fungi / Q000201:enzymology; D042845:Laccase / Q000378:metabolism*; D013329:Structure-Activity Relationship; D047090:beta-Lactams / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D002396:Catechols; D047090:beta-Lactams; D042845:Laccase