4,7-二氯苯并噻吩-2-基磺酰氨基甲基硼酸：首个具有A类、C类和D类活性的硼酸衍生β-内酰胺酶抑制剂。
4,7-Dichloro benzothien-2-yl sulfonylaminomethyl boronic acid: first boronic acid-derived beta-lactamase inhibitor with class A, C, and D activity.
作者信息
Tan Qiang, Ogawa Aimie M, Painter Ronald E, Park Young-Whan, Young Katherine, DiNinno Frank P
机构信息
Department of Medicinal Chemistry, Merck & Co., Inc., Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2010 Apr 15;20(8):2622-4. doi: 10.1016/j.bmcl.2010.02.065. Epub 2010 Feb 19.
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.
4,7-二氯-1-苯并噻吩-2-基磺酰氨基甲基硼酸（DSABA，化合物I）作为首个基于硼酸的D类β-内酰胺酶抑制剂被发现。它对OXA-40的半数抑制浓度（IC50）为5.6微摩尔。该化合物还以亚微摩尔至低微摩尔的IC50抑制A类和C类β-内酰胺酶，并与亚胺培南协同作用对抗鲍曼不动杆菌。
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