Design,synthesis and in vitro activity of quinazolone glycine transporter-1 inhibitors

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	Design,synthesis and in vitro activity of quinazolone glycine transporter-1 inhibitors
	Jiang Neng 1; Jiang Jianqin 1; Shen Jianhua2
刊名	Journal of China Pharmaceutical University
	2012
卷号	43 期号:3 页码:199-203
关键词	schizophrenia syndrome glycine transporter-1 quinazolone design synthesis
ISSN号	1000-5048
其他题名	喹唑酮类甘氨酸转运体1抑制剂的设计、合成及药理活性研究
文献子类	Article
英文摘要	Glycine transporter-1(GlyT1) is an attractive therapeutic target for schizophrenia.A series of novel quinazolone derivatives were designed and synthesized as active GlyT1 inhibitors on the basis of compound 2,4-dichloro-N-{[4-(cyclopropylmethyl)-1-(ethylsulfonyl)piperidin-4-yl]methyl}benzamide(1a,IC_(50)=92.2 nmol/L) developed by Merck & Co Inc.Preliminary results showed that all the compounds except 7e possessed GlyT1 inhibitory activity to a different extent,and that compound 7j was the most potent one within this series of compounds,possessing almost the same potency as that of compound 1a.
WOS研究方向	Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种	中文
CSCD记录号	CSCD:4568387
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/267833]
专题	药物发现与设计中心
通讯作者	Shen Jianhua
作者单位	1.School of Traditional Chinese Medicine,China Pharmaceutical University, Nanjing, Jiangsu 210009, China.; 2.Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China.
推荐引用方式 GB/T 7714	Jiang Neng,Jiang Jianqin,Shen Jianhua. Design,synthesis and in vitro activity of quinazolone glycine transporter-1 inhibitors[J]. Journal of China Pharmaceutical University,2012,43(3):199-203.
APA	Jiang Neng,Jiang Jianqin,&Shen Jianhua.(2012).Design,synthesis and in vitro activity of quinazolone glycine transporter-1 inhibitors.Journal of China Pharmaceutical University,43(3),199-203.
MLA	Jiang Neng,et al."Design,synthesis and in vitro activity of quinazolone glycine transporter-1 inhibitors".Journal of China Pharmaceutical University 43.3(2012):199-203.