Synergistic Antibacterial Activity of Meropenem and Imipenem in Combination with Diazabicyclooctane Derivatives
文献类型： 外文期刊
作者： Sun, Jian 1 ; He, Lili 1 ; Ji, Jingwen 1 ; Zhai, Lijuan 1 ; Ji, Jinbo 1 ; Ma, Xueqin 2 ; Tang, Dong 1 ; Mu, Yangxiu 1 ; Gao, Yuanyu 1 ; Wang, Lin 1 ; Yang, Haikang 1 ; Iqbal, Zafar 1 ; Yang, Zhixiang 1 ;
作者机构： 1.Ningxia Acad Agr & Forestry Sci, 590Huanghe 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： diazabicyclooctane; amidine; beta-lactamase inhibitor; antibacterial activity
期刊名称：RUSSIAN JOURNAL OF GENERAL CHEMISTRY （ 影响因子：0.779； 五年影响因子：0.697 ）
ISSN： 1070-3632
年卷期： 2022 年 92 卷 10 期
页码：
收录情况： SCI
摘要： The diazabicyclooctane (DBO) has emerged as the attractive motif for the development of new beta-lactamase inhibitors after the clinical approval of avibactam and relebactam. We are striving at improving the lactamase inhibition strength and antibacterial spectrum of the DBO derivatives. We synthesized the substituted-amidine derivatives (5a-5j) of the DBO, and determined the antibacterial efficacy of the two beta-lactam drugs i.e. imipenem and meropenem, in combination with compounds 5a-5j. All these derivatives lowered the MIC values of the imipenem and meropenem, indicating their beta-lactamase inhibition profile, however in variable strength. The best results were obtained when the compounds 5a-5j were combined with meropenem indicating the better association of these compounds with meropenem in comparison to imipenem. With meropenem, compounds 5a and 5b proved to be the most potent exhibiting the highest antibacterial efficacy against five out of ten microbial strains. Moreover, the MIC data showed that beta-lactamase inhibition strength of compounds 5a and 5b was comparable to relebactam in eight out of ten bacterial strains.
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