Bioorganic & Medicinal Chemistry 26 (2018) 2921–2927 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc Boronic acid inhibitors of the class A b-lactamase KPC-2 Jingyuan Zhou, Paul Stapleton, Shozeb Haider, Jess Healy UCL School of Pharmacy, 29-39 Brunswick Sq., London WC1N 1AX, UK article i nfo abstract Article history: The rapid rise of antimicrobial resistance is one of the greatest challenges currently facing medical Received 5 February 2018 science. The most common cause of resistance to b-lactam antibiotics is the expression of b-lactamase Revised 24 April 2018 enzymes, such as KPC-2. As such the development of novel inhibitors of KPC-2 and related enzymes is Accepted 26 April 2018 of the upmost importance. We report the design and synthesis of novel boronic acid transition state ana- Available online 27 April 2018 logs containing a 1,4-substituted 1,2,3-triazole linker based on the known inhibitor 3-nitrophenyl boro- nic acid and demonstrate that they are promising scaffolds for the development inhibitors of KPC-2 with Keywords: the ability to recover sensitivity to the antibiotic cefotaxime. KPC 2018 Elsevier Ltd. All rights reserved. Beta-lactamase Antibiotic resistance Boronic acid inhibitors 1. Introduction clinical concern and the development of novel inhibitors is of the
Bioorganic & Medicinal Chemistry – Elsevier
Published: Jul 15, 2018
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