Bioorganic & Medicinal Chemistry Letters 2010-04-15

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

Qiang Tan, Aimie M Ogawa, Ronald E Painter, Young-Whan Park, Katherine Young, Frank P DiNinno, Qiang Tan, Aimie M. Ogawa, Ronald E. Painter, Young-Whan Park, Katherine Young, Frank P. DiNinno

Index: Bioorg. Med. Chem. Lett. 20 , 2622-4, (2010)

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Abstract

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 IC(50) of 5.6 microM against OXA-40. The compound also inhibited class A and C beta-lactamases with sub to low microM IC(50), and synergized with imipenem against Acinetobacter baumannii.Copyright 2010 Elsevier Ltd. All rights reserved.