Towards calixarene-based prodrugs: Drug release and antibacterial behaviour of a water-soluble nalidixic acid/calix [4] arene ester adduct

…, C Finance, RE Duval, JB Regnouf-de-Vains

Index: Dibama, Hugues Massimba; Clarot, Igor; Fontanay, Stephane; Salem, Adel Ben; Mourer, Maxime; Finance, Chantal; Duval, Raphael E.; Regnouf-de-Vains, Jean-Bernard Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 10 p. 2679 - 2682

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Citation Number: 40

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.