The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives

被引：52

作者：

Wang, Jing ^{[1
]}

Yang, Teng ^{[2
,3
]}

Chen, Huang ^{[4
,5
]}

Xu, Yun-Nan ^{[1
]}

Yu, Li-Fang ^{[1
]}

Liu, Ting ^{[1
]}

Tang, Jie ^{[1
,6
]}

Yi, Zhengfang ^{[4
,5
]}

Yang, Cai-Guang ^{[3
]}

Xue, Wei ^{[2
]}

Yang, Fan ^{[1
]}

机构：

[1] East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, SCME, Shanghai 200062, Peoples R China

[2] Guizhou Univ, Key Lab Green Pesticide & Agr Bioengn, Ctr Res & Dev Fine Chem, Minist Educ, Guiyang 550225, Peoples R China

[3] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China

[4] East China Normal Univ, Shanghai Key Lab Regulatory Biol, Inst Biomed Sci, Shanghai 200241, Peoples R China

[5] East China Normal Univ, Sch Life Sci, Shanghai 200241, Peoples R China

[6] East China Normal Univ, SCME, Shanghai Key Lab Green Chem & Chem Proc, Shanghai 200062, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2017年 / 127卷

基金：

中国国家自然科学基金;

关键词：

Berberine derivatives; Antistaphylococcal activity; Multidrug-resistant; Cytotoxicity; RESISTANT STAPHYLOCOCCUS-AUREUS; HUMAN SERUM-ALBUMIN; MULTIFUNCTIONAL AGENTS; ANTIBACTERIAL ACTIVITY; ANTIMICROBIAL ACTIVITY; BIOLOGICAL EVALUATION; ALZHEIMERS-DISEASE; NATURAL-PRODUCT; IN-VITRO; HYBRIDS;

D O I：

10.1016/j.ejmech.2017.01.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 9, 13-disubstituted berberine derivatives have been synthesized and evaluated for the antibacterial activities against Staphylococcus aureus, including Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). Compound 20 shows the most potent activity against the growth of Newman strain, with a MIC value of 0.78 mu g/mL, which is comparable with the positive control vancomycin. In addition, compound 20, 21, and 33 are highly antistaphylococcal active against five strains of multidrug-resistant S. aureus, with MIC values of 0.78-1.56 mu g/mL. Of note, theses antibacterial active compounds have no obvious toxicity to the viability of human fibroblast (HAF) cells at the MIC concentration. (C) 2017 Elsevier Masson SAS. All rights reserved.

引用

页码：424 / 433

页数：10

共 38 条

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