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4,7-Dichloro benzothien-2-yl sulfonylaminomethyl boronic acid: First boronic acid-derived beta-lactamase inhibitor with class A, C, and D activity

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 8, 页码 2622-2624

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.065

关键词

Boronic acid; Beta-lactamase; Inhibitor; Antibiotics; OXA-40; Class D

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4,7-Dichloro-1-benzothien-2-yl sulfonylaminomethyl boronic acid (DSABA, Compound I) was discovered as the first boronic acid-based class D beta-lactamase inhibitor. It exhibited an IC50 of 5.6 mu M against OXA-40. The compound also inhibited class A and C beta-lactamases with sub to low mu M IC50, and synergized with imipenem against Acinetobacter baumannii. (C) 2010 Elsevier Ltd. All rights reserved.

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