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

被引：44

作者：

Dibama, Hugues Massimba ^{[1
]}

Clarot, Igor ^{[1
]}

Fontanay, Stephane ^{[1
]}

Ben Salem, Adel ^{[2
]}

Mourer, Maxime ^{[1
]}

Finance, Chantal ^{[1
]}

Duval, Raphael E. ^{[1
]}

Regnouf-de-Vains, Jean-Bernard ^{[1
]}

机构：

[1] Nancy Univ, SRSMC, Fac Pharm, CNRS,UMR 7565,Grp Etude Vecteurs Supramol Medicam, F-54001 Nancy, France

[2] Fac Sci, Lab Chim Appl Heterocycles Corps Gras & Polymeres, Dept Chim, Sfax 3000, Tunisia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 10期

关键词：

Calixarene; Quinolone; Nalidixic acid; Prodrug;

D O I：

10.1016/j.bmcl.2009.03.139

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2679 / 2682

页数：4

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