Technology Research Association for Next Generation Natural Products Chemistry, 2-4-7 Aomi, Koto-ku, Tokyo 135-0064, Japan.
Japan Biological Informatics Consortium (JBIC), 2-4-7 Aomi, Koto-ku, Tokyo 135-0064 Japan.
Org Lett. 2021 Jun 4;23(11):4415-4419. doi: 10.1021/acs.orglett.1c01352. Epub 2021 May 24.
We discovered JBIR-155 as a novel specific class D β-lactamase inhibitor from SoB100815Hv02. JBIR-155 consists of a 6-oxabicyclo[3.2.0]heptan-7-one skeleton and a long unsaturated alkyl chain moiety of which absolute configuration was determined by spectroscopic data, modified Mosher's method, and analyses of the relative configuration of chemically modified derivative. JBIR-155 specifically exhibited inhibitory activity against the class D β-lactamase, with an IC value of 0.36 μM.
我们从 SoB100815Hv02 中发现了 JBIR-155,这是一种新型的特异性 Class Dβ-内酰胺酶抑制剂。JBIR-155 由 6-氧杂双环[3.2.0]庚烷-7-酮骨架和长不饱和烷基链组成,其绝对构型通过光谱数据、改良的 Mosher 法和化学修饰衍生物的相对构型分析确定。JBIR-155 特异性地表现出对 Class Dβ-内酰胺酶的抑制活性,IC 值为 0.36μM。