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Boronic acid inhibitors of the class A beta-lactamase KPC-2

Zhou, J; Stapleton, P; Haider, S; Healy, J; (2018) Boronic acid inhibitors of the class A beta-lactamase KPC-2. Bioorganic & Medicinal Chemistry , 26 (11) pp. 2921-2927. 10.1016/j.bmc.2018.04.05c. Green open access

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Abstract

The rapid rise of antimicrobial resistance is one of the greatest challenges currently facing medical science. The most common cause of resistance to β-lactam antibiotics is the expression of β-lactamase enzymes, such as KPC-2. As such the development of novel inhibitors of KPC-2 and related enzymes is of the upmost importance. We report the design and synthesis of novel boronic acid transition state analogs containing a 1,4-substituted 1,2,3-triazole linker based on the known inhibitor 3-nitrophenyl boronic acid and demonstrate that they are promising scaffolds for the development inhibitors of KPC-2 with the ability to recover sensitivity to the antibiotic cefotaxime.

Type: Article
Title: Boronic acid inhibitors of the class A beta-lactamase KPC-2
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.bmc.2018.04.05c
Publisher version: http://dx.doi.org/10.1016/j.bmc.2018.04.05c
Language: English
Additional information: This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions.
Keywords: KPC, Beta-lactamase, Antibiotic resistance, Boronic acid inhibitors
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharma and Bio Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/10052039
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