Sulfonylamidine-substituted derivatives of avibactam: Synthesis and antibacterial activity

文献类型： 外文期刊

第一作者： Ji, Jingwen

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

作者机构：

期刊名称：JOURNAL OF HETEROCYCLIC CHEMISTRY （ 影响因子：2.193； 五年影响因子：1.645 ）

ISSN： 0022-152X

年卷期： 2021 年 58 卷 12 期

页码：

收录情况： SCI

摘要： Avibactam is a clinically approved non-beta-lactam based beta-lactamase inhibitor. Derivatization of this scaffold with improved inhibition profile is the demand of the day to cope with the future challenges. We successfully synthesized new derivatives of avibactam containing sulfonylamidine moieties at C2 position of the diazabicyclooctane ring. We tested in vitro antibacterial activities of newly synthesized compounds against 10 bacterial strains expressing variable beta-lactamases. All compounds did not exhibit antimicrobial profile when assayed individually; however, all compounds minimized the MIC value of the imipenem in combination. Compound 5l proved most potent against all 10 bacterial strains, and showed improved inhibition against six bacterial strains as compared with the control inhibitor, relebactam. The compound 5l may be a lead hit for future development.

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