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学科主题: 基础医学
题名:
Design, Synthesis and Biological Activities of a Series of Piperazine Pyrimidine as CCR4 Antagonists
作者: 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
发表日期: 2013-09-10
DOI: 10.7503/cjcu20120607
卷: 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:
内容类型: 期刊论文
版本: 出版稿
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56326
Appears in Collections:基础医学院_北京大学人类疾病基因研究中心_期刊论文

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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:
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.
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