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

doi:10.1016/j.ejmech.2017.01.012

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	The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives
	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-Guang3 ; Xue, Wei 2
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2017-02-15
卷号	127 页码:424-433
关键词	Berberine derivatives Antistaphylococcal activity Multidrug-resistant Cytotoxicity
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2017.01.012
文献子类	Article
英文摘要	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.
资助项目	National Key Technology RD Program[2015BAK45B00] ; National Natural Science Foundation of China[81472788] ; National Natural Science Foundation of China[81272463] ; National Natural Science Foundation of China[81661138004] ; Major State Basic Research Development Program of China[2015CB910400] ; Shanghai Science and Technology Council[14DZ0511800] ; Shanghai Science and Technology Council[14142201200] ; Laboratory of Organic Functional Molecules, Sino-French Institute of ECNU[00000000]
WOS关键词	RESISTANT STAPHYLOCOCCUS-AUREUS ; HUMAN SERUM-ALBUMIN ; MULTIFUNCTIONAL AGENTS ; ANTIBACTERIAL ACTIVITY ; ANTIMICROBIAL ACTIVITY ; BIOLOGICAL EVALUATION ; ALZHEIMERS-DISEASE ; NATURAL-PRODUCT ; IN-VITRO ; HYBRIDS
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000397172800035
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275629]
专题	药理学第三研究室中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Xue, Wei; Yang, Fan
作者单位	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
推荐引用方式 GB/T 7714	Wang, Jing,Yang, Teng,Chen, Huang,et al. The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2017,127:424-433.
APA	Wang, Jing.,Yang, Teng.,Chen, Huang.,Xu, Yun-Nan.,Yu, Li-Fang.,...&Yang, Fan.(2017).The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,127,424-433.
MLA	Wang, Jing,et al."The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 127(2017):424-433.