Towards calixarene-based prodrugs: Drug release and antibacterial behaviour of a water-soluble nalidixic acid/calix[4]arene ester adduct |
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| Authors: | Hugues Massimba Dibama Igor Clarot Stéphane Fontanay Adel Ben Salem Maxime Mourer Chantal Finance Raphaël E Duval Jean-Bernard Regnouf-de-Vains |
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| Institution: | 1. SRSMC, UMR 7565 Nancy Université–CNRS; Groupe d’Etude des Vecteurs Supramoléculaires du Médicament, Faculté de Pharmacie, 5, rue Albert Lebrun, BP 80403, 54001 Nancy Cedex, France;2. Laboratoire de Chimie Appliquée: Hétérocycles, Corps Gras et polymères. Département de Chimie, Faculté des Sciences de Sfax, 3000 Sfax, B.P. 1171, Tunisia |
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| 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. |
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