title: Towards calixarene-based prodrugs: Drug release and antibacterial behaviour of a water-soluble nalidixic acid/calix[4]arene ester adduct.
abstract: A water-soluble calixarene-based heterocyclic podand incorporating a quinolone antibiotic subunit, the nalidixic acid, was synthesised and fully characterised. Its prodrug behaviour was assessed in vitro by HPLC, demonstrating the release of the tethered quinolone in model biological conditions. Microbiological studies performed on various Gram-positive and Gram-negative reference strains showed very interesting antibacterial activities.
authors.affiliation: SRSMC, UMR Nancy Université-CNRS, France.
authors.forename: Hugues Massimba
authors.initials: HM
authors.lastname: Dibama
authors.forename: Igor
authors.initials: I
authors.lastname: Clarot
authors.forename: Stéphane
authors.initials: S
authors.lastname: Fontanay
authors.forename: Adel Ben
authors.initials: AB
authors.lastname: Salem
authors.forename: Maxime
authors.initials: M
authors.lastname: Mourer
authors.forename: Chantal
authors.initials: C
authors.lastname: Finance
authors.forename: Raphaël E
authors.initials: RE
authors.lastname: Duval
authors.forename: Jean-Bernard
authors.initials: JB
authors.lastname: Regnouf-de-Vains
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047250:Calixarenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D009268:Nalidixic Acid / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D010636:Phenols / Q000737:chemistry*; D011355:Prodrugs / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D014867:Water / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D010636:Phenols; D011355:Prodrugs; C121325:calix(4)arene; D014867:Water; D047250:Calixarenes; D009268:Nalidixic Acid