Improved synthesis and evaluation of preclinical pharmacodynamic parameters of a new monocyclic β-lactam DPI-2016

文献类型： 外文期刊

第一作者： Zhai, Lijuan

作者： Zhai, Lijuan;Sun, Jian;Ji, Jingwen;He, Lili;Zhou, Pengjuan;Tang, Dong;Ji, Jinbo;Yang, Haikang;Iqbal, Zafar;Yang, Zhixiang

作者机构：

关键词： Monobactam; Aztreonam; beta-lactams; Antibacterial

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS （ 影响因子：2.7； 五年影响因子：2.6 ）

ISSN： 0960-894X

年卷期： 2024 年 99 卷

页码：

收录情况： SCI

摘要： Monocyclic beta-lactams are stable to a number of beta-lactamases and are the focus of researchers for the development of antibacterial drugs, particularly against Enterobacterales. We recently synthesized and reported the bactericidal activity of diverse series of aztreonam appended with amidine moieties as siderophores. One of the derivatives exhibiting the highest MIC value in vitro was selected for further preclinical studies. The compound DPI2016 was reassessed for its synthetic routes and methods that were improved to find the maximum final yields aimed at large-scale synthesis. In addition, the results of the pharmacological studies were determined with reference to aztreonam. It has been found that the compound DPI-2016 showed comparable or slightly improved ADMET as well as pharmacokinetic parameters to aztreonam. It is estimated that the compound could be a potential lead for further clinical evaluation.

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