文献类型： 外文期刊
作者： Zhai, Lijuan 1 ; Sun, Jian 1 ; Ji, Jingwen 1 ; He, Lili 1 ; Gao, Yuanyu 1 ; Ji, Jinbo 1 ; Liu, Yuanbai 1 ; Mu, Yangxiu 1 ; Ma, Xueqin 2 ; 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, Coll Pharm, Shengli St, Yinchuan 750004, Ningxia, Peoples R China
关键词： diazabicyclooctane; imidates; antibacterial activity; beta-lactamase inhibitor; avibactam
期刊名称：RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY （ 影响因子：1.254； 五年影响因子：1.063 ）
ISSN： 1068-1620
年卷期：
页码：
收录情况： SCI
摘要： A series of new imidate derivatives of avibactam (diazabicyclooctane derivative) was prepared for their prospective beta-lactamase inhibition activity. The compounds (VIIa-m) were prepared through multiple synthetic steps; starting from benzyl deprotection in cyano derivative of diazabicyclooctane, sulfonation of hydroxy intermediate, and late-stage modification at C2 of the bicyclic ring to form the final compounds. The compounds were subjected to antimicrobial activity alone, as well as a combination with imipenem against ten bacterial strains expressing variable beta-lactamase(s). All the compounds did not show bactericidal behavior when tested alone, however all compounds minimized the MIC value of imipenem indicating their beta-lactamase inhibition strength, in vitro. Four compounds showed highest activity (MIC <= 0.125 mg/L), and comparable to avibactam against six bacterial species.
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