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Boronic Acid Inhibitors of the Class A β-lactamase KPC-2

Boronic Acid Inhibitors of the Class A β-lactamase KPC-2

Jingyuan Zhou, Paul Stapleton, Shozeb Haider, Jess Healy

Bioorg Med Chem. 2018 Jul 15;26(11):2921-2927.

PMID: 29784271

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	CAS Number	Price
AP475102126	(N-Boc-5-chloro-2-indolyl)boronic acid	475102-12-6	Price
LS793652	3-methoxy-2-hydroxyphenyl boronic acid		Price
LS793655	2-hydroxy-3-methylphenyl boronic acid		Price

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