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

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.

journal_name

Bioorg Med Chem Lett

authors

Tan Q,Ogawa AM,Painter RE,Park YW,Young K,DiNinno FP

doi

10.1016/j.bmcl.2010.02.065

subject

Has Abstract

pub_date

2010-04-15 00:00:00

pages

2622-4

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00265-9

journal_volume

20

pub_type

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