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学科主题: 药学
题名:
N-[2-Chloro-9H-purin-6-yl]-N-cyclopropylglycylamino acids and derivatives: Synthesis, evaluation as a class of novel analgesics, and 3D QSAR analysis
作者: Zhao, Jinghua2; Kang, Guifeng2; Wang, Wei3; Zhao, Ming1; Zhang, Xiaoyi1; Lu, Chunbo4; Mao, Wei4; Chang, Heng Wei3; Ye, Weidong4; Peng, Shiqi1,2
关键词: Substituted purine ; Analgesia ; 3D QSAR
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
发表日期: 2009-09-01
DOI: 10.1016/j.bmc.2009.07.035
卷: 17, 期:17, 页:6305-6310
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: ADENOSINE RECEPTOR AGONISTS ; A(1) RECEPTOR ; ALLOSTERIC MODULATION ; NEUROPATHIC PAIN ; GLYCINE ; ANTAGONISTS ; INHIBITORS ; AFFINITY ; LIGANDS ; BRAIN
英文摘要:

Via a five-step-reaction procedure for the preparation of 19 known N-[2-chloro-9-(tetrahydropyran-2-yl)- 9H-purin-6-yl]-N-cyclopropylglycylamino acid benzylesters (6a-s) and successive removal of 9-(tetrahydropyran- 2-yl) and benzylester groups 19 novel N-[2-chloro-9H-purin-6-yl]-N-cyclopropylglycylamino acid benzylesters (7a-s) and 19 novel N-[2-chloro-9H-purin-6-yl]-N-cyclopropylglycylamino acids (8a-s) were provided. On tail-flick mouse model the in vivo analgesic activities of these 38 novel compounds were measured and most of them were defined as good analgesics. Based on Molecular Field Analysis of the pain threshold variations of the mice receiving 48 compounds in terms of the descriptors proton and methyl an equation was established. The data points (n), correlation coefficient (r), and square correlation coefficient (r(2)) of this equation were 48, 0.923, and 0.852, respectively. Using this equation pain threshold variations of 9 compounds were predicted and the errors ranged from 1.71 to 8.92. (C) 2009 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: KZ200810025010 ; 2008ZX09401-002 ; 30672513
项目资助者: PHR ; National Natural Science Foundation of China
WOS记录号: WOS:000269029100020
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56133
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
2.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
3.CS Bio Co, Menlo Pk, CA 94025 USA
4.Zhejiang Med Co LTD, Xinchang 312500, Zhejiang, Peoples R China

Recommended Citation:
Zhao, Jinghua,Kang, Guifeng,Wang, Wei,et al. N-[2-Chloro-9H-purin-6-yl]-N-cyclopropylglycylamino acids and derivatives: Synthesis, evaluation as a class of novel analgesics, and 3D QSAR analysis[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2009,17(17):6305-6310.
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