Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold

doi:10.1016/j.bmcl.2015.07.030

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	Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold
	Deng, Xinxian 2,3,4; Guo, Lin 1; Xu, Lili 2,3,4; Zhen, Xuechu 5,6; Yu, Kunqian1 ; Zhao, Weili 2,3,4; Fu, Wei 2,3,4
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2015-09-15
卷号	25 期号:18 页码:3970-3974
关键词	5-HT2A receptor antagonist Quinazoline derivatives Synthesis Molecular docking
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2015.07.030
文献子类	Article
英文摘要	A series of compounds with quinazoline scaffold were designed, synthesized and evaluated as novel potent 5-HT2A receptor ligands. N-(4-Chlorophenyl)-2-(piperazin-1-yl)quinazolin-4-amine (5o) has a K-i value of 14.04 +/- 0.21 nM, with a selectivity more than 10,000 fold over 5-HT1A receptors (D-1 and D-2-like receptors). The functional assay showed that this compound is an antagonist to 5-HT2A receptor with an IC50 value of 1.66 mu M. (C) 2015 Elsevier Ltd. All rights reserved.
资助项目	National Natural Science Foundation of China[81172919] ; National Natural Science Foundation of China[81130023] ; National Natural Science Foundation of China[81473136] ; National Basic Research Plan (973) of the Ministry of Science and Technology of China[2011CB5C4403] ; Priority Academic Program Development of Jiangsu Higher Education Institutes (PAPD)[00000000]
WOS关键词	SITE-DIRECTED MUTAGENESIS ; DRUG DISCOVERY ; BINDING-SITE ; SEROTONIN ; DERIVATIVES ; IDENTIFICATION ; ANTAGONIST ; INHIBITORS ; AGONIST ; DISRUPTION
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000359747700042
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276396]
专题	药理学第二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药物发现与设计中心
通讯作者	Zhen, Xuechu
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China 2.Fudan Univ, Dept Med Chem, Shanghai 201203, Peoples R China; 3.Fudan Univ, Key Lab Smart Drug Delivery, Minist Educ, Shanghai 201203, Peoples R China; 4.Fudan Univ, Sch Pharm, PLA, Shanghai 201203, Peoples R China; 5.Soochow Univ, Jiangsu Key Lab Translat Res & Therapy Neuropsych, Coll Pharmaceut Sci, Suzhou 215123, Jiangsu, Peoples R China; 6.Soochow Univ, Dept Pharmacol, Coll Pharmaceut Sci, Suzhou 215123, Jiangsu, Peoples R China;
推荐引用方式 GB/T 7714	Deng, Xinxian,Guo, Lin,Xu, Lili,et al. Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2015,25(18):3970-3974.
APA	Deng, Xinxian.,Guo, Lin.,Xu, Lili.,Zhen, Xuechu.,Yu, Kunqian.,...&Fu, Wei.(2015).Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,25(18),3970-3974.
MLA	Deng, Xinxian,et al."Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 25.18(2015):3970-3974.