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Substituted-Amidine Functionalized Monocyclic beta-Lactams: Synthesis and In Vitro Antibacterial Profile

文献类型： 外文期刊

作者： He, Lili 1 ; Zhai, Lijuan 1 ; Sun, Jian 1 ; Ji, Jingwen 1 ; Ji, Jinbo 1 ; Liu, Yuanbai 1 ; Mu, Yangxiu 1 ; Gao, Yuanyu 1 ; T 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.Kalay Univ, Dept Chem, Kalay 03044, Sagaing Region, Myanmar

期刊名称：JOURNAL OF CHEMISTRY （ 影响因子：2.506； 五年影响因子：2.726 ）

ISSN： 2090-9063

年卷期： 2021 年 2021 卷

页码：

收录情况： SCI

摘要： Background. Owing to the intrinsic stability against common beta-lactamases and metallo-lactamases, monobactams gathered special attention in antibiotic drug development. However, so far, aztreonam is the only monobactam approved by FDA for clinical use. We designed new derivatives of aztreonam to enhance its antibacterial efficacy. Methods. We synthesized a series of monocyclic beta-lactams by modifying mainly at the C3 position of azetidinone ring. NH2 group at C3 of azetidinone was attached to thiazole and thiadiazole which in turn was linked to nitrogenous heterocyclic rings via amidine moieties. We then investigated the in vitro antibacterial activities of synthesized compounds against ten bacterial strains of clinical interest in comparison to aztreonam and ceftazidime. Results. All compounds showed improved antibacterial activities against tested strains compared to reference drugs. Compounds 14d and 14e were most potent and showed the highest potency against all bacterial strains, with MIC values ranging from 0.25 mu g/mL to 8 mu g/mL, as compared to aztreonam (MIC 16 mu g/mL to >64 mu g/mL) and ceftazidime (MIC >64 mu g/mL). These compounds (14d and 14e) may be valuable lead targets against multidrug-resistant Gram-negative bacteria.

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