IR@PKUHSC  > 北京大学基础医学院  > 北京大学人类疾病基因研究中心
学科主题基础医学
Design, Synthesis and Biological Activities of a Series of Piperazine Pyrimidine as CCR4 Antagonists
Gong Hong-Wei1,2,3; Qi Hui4; Sun Wei1; Jiang Dan3; Xia Jun-Hai3; Yang Xiao-Hong1; Wang Ying4; Li Song3
关键词CCR4 antagonists Chemokine-like factor 1 (CKLF1) Thymus and activation regulated chemokine (TARC) Macrophage-derived chemokine (MDC) Inflammatory disease
刊名CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
2013-09-10
DOI10.7503/cjcu20120607
34期:9页:2131-2138
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Multidisciplinary
研究领域[WOS]Chemistry
关键词[WOS]AIRWAY INFLAMMATION ; CHEMOKINE ; POTENT ; OPTIMIZATION ; HYPERRESPONSIVENESS ; ASTHMA ; THYMUS ; CELLS ; MICE
英文摘要

CC chemokine receptor 4( CCR4) is a pivotal factor in the development of allergic inflammations, such as asthma, dermatitis and rhinitis. CCR4 antagonists have a huge potential in the therapeutics of the allergic diseases, and BMS-397 is the most potent CCR4 antagonists in the reported compounds. The structure-activity relationship of BMS-397 was studied and the large influence of the groups of pyridine and piperidine on the activity led us to modify these two sites. A series of piperazine pyrimidine derivatives was designed and synthesized. Their structures were characterized by H-1 NMR, C-13 NMR, MS and elemental analysis. The activities of all the newly synthesized compounds were evaluated using a chemotaxis inhibition assay. The results of biological activity experiment show that compound 8a was more potent than BMS-397. In the murine rhinitis model, budesonide was used as the calibration or comparison standard to assess the relative efficacy of compound 8a. The results show that compound 8a was more effective than budesonide, revealed excellent affinity to N-terminal of CCR4, and the apparent binding constant of CZE experiment result was (3. 6179 +/- 0. 5976) x 10(4) L/mol.

语种中文
WOS记录号WOS:000328926400019
Citation statistics
Cited Times:2[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
版本出版稿
条目标识符http://ir.bjmu.edu.cn/handle/400002259/56326
Collection北京大学基础医学院_北京大学人类疾病基因研究中心
作者单位1.Jilin Univ, Sch Publ Hlth, Changchun 130021, Peoples R China
2.Jilin Univ, Sch Pharmaceut Sci, Changchun 130021, Peoples R China
3.Acad Mil Med Sci, Beijing Inst Pharmacol & Toxicol, Beijing 100850, Peoples R China
4.Peking Univ, Ctr Human Dis Genom, Beijing 100191, Peoples R China
Recommended Citation
GB/T 7714
Gong Hong-Wei,Qi Hui,Sun Wei,et al. Design, Synthesis and Biological Activities of a Series of Piperazine Pyrimidine as CCR4 Antagonists[J]. CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,2013,34(9):2131-2138.
APA Gong Hong-Wei.,Qi Hui.,Sun Wei.,Jiang Dan.,Xia Jun-Hai.,...&Li Song.(2013).Design, Synthesis and Biological Activities of a Series of Piperazine Pyrimidine as CCR4 Antagonists.CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,34(9),2131-2138.
MLA Gong Hong-Wei,et al."Design, Synthesis and Biological Activities of a Series of Piperazine Pyrimidine as CCR4 Antagonists".CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE 34.9(2013):2131-2138.
Files in This Item: Download All
File Name/Size DocType Version Access License
哌嗪嘧啶类CCR4拮抗剂的设计、合成及生(1281KB)期刊论文出版稿开放获取CC BY-NC-SAView Download
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
谷歌学术
谷歌学术Similar articles in
[Gong Hong-Wei]'s Articles
[Qi Hui]'s Articles
[Sun Wei]'s Articles
百度学术
百度学术Similar articles in
[Gong Hong-Wei]'s Articles
[Qi Hui]'s Articles
[Sun Wei]'s Articles
必应学术
必应学术Similar articles in
[Gong Hong-Wei]'s Articles
[Qi Hui]'s Articles
[Sun Wei]'s Articles
Terms of Use
No data!
Social Bookmark/Share
File name: 哌嗪嘧啶类CCR4拮抗剂的设计、合成及生物活性.pdf
Format: Adobe PDF
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.