Synthesis and beta-Lactamase Inhibition Activity of Diazabicyclooctane Derivatives in Combination with Imipenem
文献类型： 外文期刊
作者： He, L. 1 ; Ji, J. 1 ; Yang, H. 1 ; Sun, J. 1 ; Zhai, L. 1 ; Ma, X. 2 ; Tang, D. 1 ; Mu, Y. 1 ; Wang, L. 1 ; Iqbal, Z. 1 ; Yang, Z. 1 ;
作者机构： 1.Ningxia Acad Agr & Forestry Sci, Yinchuan 750002, Peoples R China
2.Ningxia Med Univ, Coll Pharm, Yinchuan 750004, 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：0.9； 五年影响因子：0.7 ）
ISSN： 1070-3632
年卷期： 2022 年 92 卷 12 期
页码：
收录情况： SCI
摘要： beta-Lactamase inhibition is an integral part of combination therapy to tackle antibiotic resistance. So far clavulanic acid is the only beta-lactamase inhibitor that exhibits oral bioavailability. We synthesized new diazabicyclooctane derivatives by replacing the SO3H with CHXCOOR moiety. The antibacterial activity of these compounds, in combination with imipenem, was determined against ten bacterial strains. All compounds showed variable profile of beta-lactamase inhibition, however, most of the compounds were potent against K. pneumoniae 700603 with two- to six-fold minimization of MIC value of imipenem.
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