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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.
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https://hal.univ-lorraine.fr/hal-01651216
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Submitted on : Tuesday, November 28, 2017 - 5:52:29 PM
Last modification on : Wednesday, December 1, 2021 - 2:35:48 PM

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Hugues Massimba Dibama, Igor Clarot, Stéphane Fontanay, Adel Ben Salem, Maxime Mourer, et al.. Towards calixarene-based prodrugs: Drug release and antibacterial behaviour of a water-soluble nalidixic acid/calix[4]arene ester adduct. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2009, 19 (10), pp.2679 - 2682. ⟨10.1016/j.bmcl.2009.03.139⟩. ⟨hal-01651216⟩

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