title: Molecular drug-organiser: synthesis, characterization and biological evaluation of penicillin V and/or nalidixic acid calixarene-based podands.
abstract: Two well-known antibiotic heterocycles, the 'quinolone' nalidixic acid and the β-lactam penicillin V, active at different levels of the bacterial growth process, have been attached via an ether-ester junction to the p-tert-butylcalix[4]arene lower rim, in alternate position. The resulting hydrophobic molecular drug-organisers were fully characterized, and evaluated over two Gram negative and three Gram positive reference strains, using disk diffusion assays with disks impregnated with solution of title compound in pure DMSO. An interesting activity was observed over Staphylococcus aureus ATCC 25923 with the dis-symmetrical podand incorporating one penicillin and one nalidixic ester moieties.
authors.affiliation: SRSMC, UMR 7565 Nancy Université, CNRS, équipe GEVSM, Faculté de Pharmacie, 5, rue Albert Lebrun, BP 80403, 54001 Nancy Cedex, France.
authors.forename: Adel
authors.initials: A
authors.lastname: Ben Salem
authors.forename: Guillaume
authors.initials: G
authors.lastname: Sautrey
authors.forename: Stéphane
authors.initials: S
authors.lastname: Fontanay
authors.forename: Raphaël E
authors.initials: RE
authors.lastname: Duval
authors.forename: Jean-Bernard
authors.initials: JB
authors.lastname: Regnouf-de-Vains
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D001424:Bacterial Infections / Q000188:drug therapy; D047250:Calixarenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008826:Microbial Sensitivity Tests; D009268:Nalidixic Acid / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010404:Penicillin V / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects
chemical_list: D000900:Anti-Bacterial Agents; D047250:Calixarenes; D009268:Nalidixic Acid; D010404:Penicillin V
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