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Unique spirocyclopiperazinium salt. Part 4: Modification of dispirocyclopiperazinium (DSPZ) salts as analgesics
Li, Ang; Wang, Xin; Yue, Cal-Qin; Ye, Jia; Li, Chang-Ling; Li, Run-Tao
关键词dispirocyclopiperazinium salts analgesic structure-activity relationship synthesis
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2007-09-15
DOI10.1016/j.bmcl.2007.07.010
17期:18页:5078-5081
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]BIOLOGICAL-ACTIVITIES ; PRODRUGS
英文摘要

In order to improve the analgesic activity of lead compound 7a, two series of dispirocyclopiperaziniurn (DSPZ) salts 9a-h, 10a-e and compounds 14, 15 were synthesized and evaluated for their in vivo analgesic activity both by acetic acid induced writhing test and hot plate test. Compounds 9h, 14, and 15 exhibited better analgesic activities than 7a. Several important structure-activity relationships were revealed from this study: (1) the introduction of aryl group would obviously improve the activity; (2) it was favorable to enhance the analgesic activity and reduce the toxicity to incorporate alkyl group with suitable length in the molecule; (3) carbamate analogues displayed lower toxicity than carboxylic ester analogues; (4) hydroxylation and chlorination of lead compound could increase the analgesic activity in hot plate test. (c) 2007 Elsevier Ltd. All rights reserved.

语种英语
WOS记录号WOS:000249510900013
引用统计
被引频次:6[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/400002259/58874
专题北京大学药学院_化学生物学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100083, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100083, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Li, Ang,Wang, Xin,Yue, Cal-Qin,et al. Unique spirocyclopiperazinium salt. Part 4: Modification of dispirocyclopiperazinium (DSPZ) salts as analgesics[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2007,17(18):5078-5081.
APA Li, Ang,Wang, Xin,Yue, Cal-Qin,Ye, Jia,Li, Chang-Ling,&Li, Run-Tao.(2007).Unique spirocyclopiperazinium salt. Part 4: Modification of dispirocyclopiperazinium (DSPZ) salts as analgesics.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,17(18),5078-5081.
MLA Li, Ang,et al."Unique spirocyclopiperazinium salt. Part 4: Modification of dispirocyclopiperazinium (DSPZ) salts as analgesics".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 17.18(2007):5078-5081.
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