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Bioorg Med Chem Lett. 2011 Jun 1;21(11):3282-5. doi: 10.1016/j.bmcl.2011.04.027. Epub 2011 Apr 13.

The identification of new metallo-β-lactamase inhibitor leads from fragment-based screening.

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The University of Queensland, School of Chemistry and Molecular Biosciences, Brisbane, QLD 4072, Australia.


The emergence of metallo-β-lactamases (MBLs) capable of hydrolysing a broad spectrum of β-lactam antibiotics is particularly concerning for the future treatment of bacterial infections. This work describes the discovery of lead compounds for the development of new inhibitors using a competitive colorimetric assay based on the chromogenic cephalosporin CENTA, and a 500 compound Maybridge™ library suitable for fragment-based screening. The interactions between identified inhibitory fragments and the active site of the MBL from Klebsiella pneumoniae and Pseudomonas aeruginosa were probed by in silico docking studies.

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