Synthesis, Antibacterial and Pharmacokinetic Evaluation of Novel Derivatives of Harmine N-9-Cinnamic Acid

文献类型： 外文期刊

第一作者： Liang, Yan

作者： Liang, Yan;He, Dian;Wang, Zhen;Zhou, Deshun;Li, Junshuai;Tang, Lei

作者机构：

关键词： harmine; synthesis; antibacterial activity; pharmacokinetics

期刊名称：MOLECULES （ 影响因子：4.412； 五年影响因子：4.588 ）

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年卷期： 2021 年 26 卷 16 期

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收录情况： SCI

摘要： A series of 16 new derivatives of harmine N-9-Cinnamic acid were synthesized and fully characterized using NMR and MS. The in vitro antibacterial evaluation revealed that most of the synthesized harmine derivatives displayed better antibacterial activities against Gram-positive strains (S. aureus, S. albus and MRSA) than Gram-negative strains (E. coli and PA). In particular, compound 3c showed the strongest bactericidal activity with a minimum inhibitory concentration of 13.67 mu g/mL. MTT assay showed that compound 3c displayed weaker cytotoxicity than harmine with IC50 of 340.30, 94.86 and 161.67 mu mol/L against WI-38, MCF-7 and HepG2 cell lines, respectively. The pharmacokinetic study revealed that the distribution and elimination of 3c in vivo were rapid in rats with an oral bioavailability of 6.9%.

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