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.
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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.
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