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Substituted-amidine derivatives of diazabicyclooctane as prospective beta-lactamase inhibitors

文献类型： 外文期刊

作者： Liu, Yuanbai 1 ; Ji, Jingwen 1 ; Sun, Jian 1 ; He, Lili 1 ; Gao, Yuanyu 1 ; Zhai, Lijuan 1 ; Ji, Jinbo 1 ; Ma, Xueqin 2 ; Mu, Yangxiu 1 ; Tang, Dong 1 ; Yang, Haikang 1 ; Iqbal, Zafar 1 ; Yang, Zhixiang 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, Dept Pharm, Shengli St, Yinchuan 750004, Ningxia, Peoples R China

关键词： Heterocycles; Antibiotics; Bioorganic chemistry; Amidine; Lactamase inhibition

期刊名称：MONATSHEFTE FUR CHEMIE （ 影响因子：1.613； 五年影响因子：1.557 ）

ISSN： 0026-9247

年卷期： 2022 年 153 卷 3 期

页码：

收录情况： SCI

摘要： Discovery of beta-lactamase inhibitors is a continuous process due to inherent capability of resistance in bacteria against existing inhibitors. Diazabicyclooctane ring is a non-beta-lactam motif capable of inhibiting the beta-lactamases. As part of our efforts, we synthesized a series of diazabicyclooctane derivatives where C2 position of the bicyclic ring is linked with various substituted-amidine moieties. The newly synthesized compounds, alone and in combination with meropenem, were tested against ten bacterial strains for their antibacterial activity in vitro. All compounds did not show antibacterial tendency when tested alone (MIC > 64 mg/dm(3)) however, showed antibacterial activity in combination with meropenem. All compounds enhanced the potency of meropenem (MIC 2-4 mg/dm(3)) with MIC values ranging from < 0.125 to 1 mg/dm(3) indicating their prospective beta-lactamase inhibition capability. One derivative proved to be the most potent among all, and is comparable to avibactam, against eight out of ten bacterial strains.

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