Synthesis,Characterization, and Biological Evaluation as Antibacterial Agents of Water‐Soluble Calix[4]arenes and Phenol Derivatives Incorporating Carboxylate Groups |
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| Authors: | Maxime Mourer Stéphane Fontanay Raphaël E Duval Jean‐Bernard Regnouf‐de‐Vains |
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| Institution: | 1. SRSMC, UMR 7565 Université de Lorraine?–?CNRS, Groupe d'Etude des Vecteurs Supramoléculaires du Médicament, Faculté de Pharmacie, 5, rue Albert Lebrun, BP 80403, F‐54001 Nancy Cedex (phone: +33‐3‐83682315;2. fax: +33‐3‐83682345) |
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| Abstract: | As part of specific investigations dedicated to the building of a chemical library of calixarenes with anti‐infective properties, some H2O‐soluble calix4]arene derivatives incorporating carboxylate groups at the upper rim and heterocycles at the lower rim have been prepared and characterized as have their constitutive functional monomers. In vitro antibacterial testing against Gram‐positive and Gram‐negative reference strains shows that the derivative with two 5,5′‐dicarboxylated 2,2′‐bithiazole subunits in alternate positions at the lower rim displays an activity at ca. 70 μM (128 μg/ml) on S. aureus ATCC 29213. |
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| Keywords: | Calixarenes Bipyridines Bithiazoles Antibacterial activity |
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