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A class of novel conjugates of substituted purine and Gly-AA-OBzl: Synthesis and evaluation of orally analgesic activity
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
2010-10-15
DOI10.1016/j.bmcl.2009.05.077
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
WOS记录号WOS:000281963700045
引用统计
被引频次:1[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/64133
专题北京大学药学院
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
推荐引用方式
GB/T 7714
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.
APA Kang, Guifeng.,Zhao, Ming.,Zhang, Xiaoyi.,Peng, Li.,Li, Chunbo.,...&Peng, Shiqi.(2010).A class of novel conjugates of substituted purine and Gly-AA-OBzl: Synthesis and evaluation of orally analgesic activity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,20(20),6157-6160.
MLA Kang, Guifeng,et al."A class of novel conjugates of substituted purine and Gly-AA-OBzl: Synthesis and evaluation of orally analgesic activity".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 20.20(2010):6157-6160.
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