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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

The Inhibition of Extended Spectrum β-Lactamases: Hits and Leads

Author(s): Davide Farina, Francesca Spyrakis, Alberto Venturelli, Simon Cross, Donatella Tondi and Maria Paola Costi

Volume 21 , Issue 12 , 2014

Page: [1405 - 1434] Pages: 30

DOI: 10.2174/09298673113206660323

Price: $65


The ongoing emergence of bacterial strains resistant to even third- and fourth-generation β-lactam antibiotics is one of the most pressing and challenging issues in clinical therapy. Furthermore, under the pressure of antibiotics used ubiquitously over the last 80 years, functional mutations and new resistances are continuously increasing. Therefore, new drugs and new approaches to the infections produced by multidrug-resistant Gram-negative bacteria are categorically necessary and expected by the scientific community. This review describes the most deleterious known extended-spectrum β- lactamases and the molecules now available for targeting bacterial infections. The active-site chemical and geometric properties that are potentially exploitable for the design of both broad-spectrum and selective compounds are described.

Keywords: β-lactam antibiotics, β-lactamase binding site, β-lactamase inhibitors, carbapenemase, extended spectrum β- lactamases, molecular interaction fields, resistance.

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