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Synthesis, Characterization, and Biological Evaluation as Antibacterial Agents of Water‐Soluble Calix[4]arenes and Phenol Derivatives Incorporating Carboxylate Groups
Author(s) -
Mourer Maxime,
Fontanay Stéphane,
Duval Raphaël E.,
RegnoufdeVains JeanBernard
Publication year - 2012
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.201200044
Subject(s) - carboxylate , calixarene , chemistry , antibacterial activity , phenol , derivative (finance) , in vitro , monomer , combinatorial chemistry , antimicrobial , stereochemistry , phenols , organic chemistry , polymer , bacteria , molecule , biochemistry , biology , financial economics , genetics , economics
Abstract As part of specific investigations dedicated to the building of a chemical library of calixarenes with anti‐infective properties, some H 2 O‐soluble calix[4]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 μ M (128 μg/ml) on S. aureus ATCC 29213.