Amidine Derivatives of Avibactam: Synthesis and In Vitro beta-Lactamase Inhibition Activity

文献类型： 外文期刊

第一作者： Gao, Yuanyu

作者： Gao, Yuanyu;Liu, Yuanbai;Iqbal, Zafar;Sun, Jian;Ji, Jinbo;Zhai, Lijuan;Tang, Dong;Ji, Jingwen;He, Lili;Mu, Yangxiu;Yang, Haikang;Yang, Zhixiang;Gao, Yuanyu

作者机构：

关键词： Antibiotics; Amidine; β -lactamase inhibitors; synthetic methods; diazabicyclooctane; synergy

期刊名称：CHEMISTRYSELECT （ 影响因子：2.109； 五年影响因子：2.054 ）

ISSN： 2365-6549

年卷期： 2021 年 6 卷 5 期

页码：

收录情况： SCI

摘要： Avibactam is a non-beta-lactam based second generation beta-lactamase inhibitor containing diazabicyclooctane (DBO) ring as the beta-lactam mimic. We substituted C2 position of DBO scaffold by a number of amidine derivatives to form water soluble final compounds A1-A14. The synthesized compounds were evaluated for their antibacterial and synergistic activity in combination with an antibiotic in vitro. The compounds, were tested against ten bacterial strains alone and in combination with existing antibiotic, meropenem. All compounds didn't show antibacterial activity when alone (MIC,>128 mu M), however exhibited moderate to good synergistic activity in the presence of meropenem by lowering its MIC values. Compound A7 proved the most potent among other counterparts against all bacterial species with MIC from <0.29 mu M to 2.34 mu M, and showed comparable or improved activity to avibactam against eight bacterial strains. Compound A7 may prove a lead for next level in vivo and clinical studies.

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