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N-[2-Chloro-9H-purin-6-yl]-N-cyclopropylglycylamino acids and derivatives: Synthesis, evaluation as a class of novel analgesics, and 3D QSAR analysis
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
2009-09-01
DOI10.1016/j.bmc.2009.07.035
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
资助者PHR ; National Natural Science Foundation of China ; PHR ; National Natural Science Foundation of China
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
资助者PHR ; National Natural Science Foundation of China ; PHR ; National Natural Science Foundation of China
WOS记录号WOS:000269029100020
引用统计
被引频次:4[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/400002259/56133
专题北京大学药学院
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
推荐引用方式
GB/T 7714
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.
APA Zhao, Jinghua.,Kang, Guifeng.,Wang, Wei.,Zhao, Ming.,Zhang, Xiaoyi.,...&Peng, Shiqi.(2009).N-[2-Chloro-9H-purin-6-yl]-N-cyclopropylglycylamino acids and derivatives: Synthesis, evaluation as a class of novel analgesics, and 3D QSAR analysis.BIOORGANIC & MEDICINAL CHEMISTRY,17(17),6305-6310.
MLA Zhao, Jinghua,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".BIOORGANIC & MEDICINAL CHEMISTRY 17.17(2009):6305-6310.
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