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beta-Lactamase inhibition profile of new amidine-substituted diazabicyclooctanes

文献类型： 外文期刊

作者： Iqbal, Zafar 1 ; Zhai, Lijuan 1 ; Gao, Yuanyu 1 ; Tang, Dong 1 ; Ma, Xueqin 2 ; Ji, Jinbo 1 ; Sun, Jian 1 ; Ji, Jingwen 1 ;

作者机构： 1.Ningxia Acad Agr & Forestry Sci, Ningxia Ctr Organ Synth & Engn Technol, 590 Huanghe East Rd, Yinchuan 750002, Ningxia, Peoples R China

2.Ningxia Med Univ, Coll Pharm, Shengli St, Yinchuan 750004, Ningxia, Peoples R China

关键词： amidine; antibacterial activity; beta-lactamase inhibitors; diazabicyclooctane; synthesis

期刊名称：BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY （ 影响因子：2.622； 五年影响因子：2.406 ）

ISSN： 1860-5397

年卷期： 2021 年 17 卷

页码：

收录情况： SCI

摘要： The diazabicyclooctane (DBO) scaffold is the backbone of non-?-lactam-based second generation ?-lactamase inhibitors. As part of our efforts, we have synthesized a series of DBO derivatives A1?23 containing amidine substituents at the C2 position of the bicyclic ring. These compounds, alone and in combination with meropenem, were tested against ten bacterial strains for their anti-bacterial activity in vitro. All compounds did not show antibacterial activity when tested alone (MIC 64 mg/L), however, they exhibited a moderate inhibition activity in the presence of meropenem by lowering its MIC values. The compound A12 proved most potent among the other counterparts against all bacterial species with MIC from <0.125 mg/L to 2 mg/L, and is comparable to avibactam against both E. coli strains with a MIC value of <0.125 mg/L.

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