Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral kappa-opioid receptor agonists

doi:10.1016/j.bmc.2016.05.002

	Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral kappa-opioid receptor agonists
	Guo, Ting 2; Gan, Zongjie 2,3; Chen, Jie 1; Wang, Dechuan 2; He, Ling 4; Song, Qiao 2,3; Xu, Yungen 2,3
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2016-07-01
卷号	24 期号:13 页码:2964-2970
关键词	Tetrahydroisoquinoline quaternary derivatives Peripheral kappa-Opioid receptor agonists
ISSN号	0968-0896
DOI	10.1016/j.bmc.2016.05.002
文献子类	Article
英文摘要	A novel series of tetrahydroisoquinoline quaternary derivatives 4 were synthesized as peripheral kappa-opioid receptor agonists. All the target compounds were evaluated in kappa-opioid receptor binding assays, and compounds 4l, 4m, and 4n exhibited high affinity for kappa-opioid receptor. Furthermore, compound 4l (kappa K-i = 0.94 nM) produced potent antinociceptive activity in the mouse acetic acid-induced writhing assay, with lower sedative side effects than the parent compound MB-1c. (C) 2016 Elsevier Ltd. All rights reserved.
资助项目	National Natural Science Foundation of China[81072520] ; Natural Science Foundation of Jiangsu Province, China[BK2010435]
WOS关键词	BLOOD-BRAIN-BARRIER ; LIMITED ACCESS ; AGENTS ; SELECTIVITY ; ICI-204448 ; DEPENDENCE
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000377468400012
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275977]
专题	中国科学院上海药物研究所
通讯作者	Xu, Yungen
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China; 3.China Pharmaceut Univ, Jiangsu Key Lab Drug Design & Optimizat, Nanjing 210009, Jiangsu, Peoples R China; 4.China Pharmaceut Univ, Dept Pharmacol, Nanjing 210009, Jiangsu, Peoples R China
推荐引用方式 GB/T 7714	Guo, Ting,Gan, Zongjie,Chen, Jie,et al. Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral kappa-opioid receptor agonists[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2016,24(13):2964-2970.
APA	Guo, Ting.,Gan, Zongjie.,Chen, Jie.,Wang, Dechuan.,He, Ling.,...&Xu, Yungen.(2016).Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral kappa-opioid receptor agonists.BIOORGANIC & MEDICINAL CHEMISTRY,24(13),2964-2970.
MLA	Guo, Ting,et al."Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral kappa-opioid receptor agonists".BIOORGANIC & MEDICINAL CHEMISTRY 24.13(2016):2964-2970.