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学科主题: 药学
题名:
A class of novel conjugates of substituted purine and Gly-AA-OBzl: Synthesis and evaluation of orally analgesic activity
作者: Kang, Guifeng2; Zhao, Ming1; Zhang, Xiaoyi1; Peng, Li1; Li, Chunbo3; Mao, Wei3; Ye, Weidong3; Peng, Shiqi1,2
关键词: Substituted purine ; Gly-AA-OBzl ; Conjugate ; Analgesia ; 3D QSAR
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2010-10-15
DOI: 10.1016/j.bmcl.2009.05.077
卷: 20, 期:20, 页:6157-6160
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: ADENOSINE RECEPTOR AGONISTS ; A(1) RECEPTOR ; ALLOSTERIC MODULATION ; NEUROPATHIC PAIN ; GLYCINE ; BRAIN
英文摘要:

Aimed at the chemotherapy of chronic pain two kinds of analgesic pharmacophores, substituted purine and Gly-AA-OBzl, were coupled via a five-step-reaction procedure and 19 novel conjugates N-[2-chloro-9-(tetrahydropyran-2-yl)-9H-purin-6-yl]-N-cyclopropylglycylamino acid benzylesters were provided. On mouse-tail flick model their in vivo analgesic activities were assayed. The results indicate that introducing Gly-OC(2)H(5) into the 6-position of the substituted purine leads to ambiguous increase of the analgesic activity, while introducing Gly-AA-OBzl into this position leads to significant increase of the analgesic activity. (C) 2010 Published by Elsevier Ltd.

语种: 英语
所属项目编号: 2008ZX09401-002 ; 30672513
项目资助者: PHR (IHLB) of China ; National Natural Science Foundation of China
WOS记录号: WOS:000281963700045
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/64133
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Zhejiang Med Co Ltd, Xinchang 312500, Zhejiang, Peoples R China
2.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
3.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Kang, Guifeng,Zhao, Ming,Zhang, Xiaoyi,et al. A class of novel conjugates of substituted purine and Gly-AA-OBzl: Synthesis and evaluation of orally analgesic activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2010,20(20):6157-6160.
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