Design and synthesis of 3-isoxazolidone derivatives as new Chlamydia trachomatis inhibitors.

Bioorg Med Chem Lett

Univ Paris Diderot, Sorbonne Paris Cité, ITODYS, UMR 7086, CNRS, 15 rue Jean-Antoine de Baïf, F-75205 Paris, France. Electronic address:

Published: August 2014

Chlamydia trachomatis (Ct) is a bacterial human pathogen responsible for the development of trachoma, the worldwide infection leading to blindness, and is also a major cause of sexually transmitted diseases. As iron is an essential metabolite for this bacterium, iron depletion presents a promising strategy to limit Ct proliferation. The aim of this study is to synthesize 3-isoxazolidone derivatives bearing known chelating moieties in an attempt to develop new bactericidal anti-Chlamydiaceae molecules. We have investigated the paths by which these new compounds affect Ct serovar L2 development in HeLa cells, in the presence or absence of exogenously added iron. The iron-chelating properties of these molecules were also determined. Our data reveal important bactericidal effects which are distinguishable from those due to iron chelation.

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http://dx.doi.org/10.1016/j.bmcl.2014.06.056DOI Listing

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Design and synthesis of 3-isoxazolidone derivatives as new Chlamydia trachomatis inhibitors.

Bioorg Med Chem Lett

August 2014

Univ Paris Diderot, Sorbonne Paris Cité, ITODYS, UMR 7086, CNRS, 15 rue Jean-Antoine de Baïf, F-75205 Paris, France. Electronic address:

Chlamydia trachomatis (Ct) is a bacterial human pathogen responsible for the development of trachoma, the worldwide infection leading to blindness, and is also a major cause of sexually transmitted diseases. As iron is an essential metabolite for this bacterium, iron depletion presents a promising strategy to limit Ct proliferation. The aim of this study is to synthesize 3-isoxazolidone derivatives bearing known chelating moieties in an attempt to develop new bactericidal anti-Chlamydiaceae molecules.

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