Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists
文献类型：期刊论文
| 作者 | Liu, Yang2,3; Zhang, Qing4 ; Chen, Lin-Hai5; Yang, Hui1; Lu, Wei2,3; Xie, Xin1,4; Nan, Fa-Jun5
|
| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2016-06 |
| 卷号 | 7期号:6页码:579-583 |
| 关键词 | GPR84 agonists 2-alkylpyrimidine-4,6-diol 6-alkylpyridine-2,4-diol structural modification |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/acsmedchemlett.6b00025 |
| 文献子类 | Article |
| 英文摘要 | A series of alkylpyrimidine-4,6-diol derivatives were designed and synthesized as novel GRP84 agonists based on a high-throughput screening (FITS) hit 1, 6-Nonylpyridine-2,4-diol was identified as the most potent agonist of GPR84 reported so far, with an EC50 of 0.189 nM. These novel GPR84 agonists will provide valuable tools for the study of the physiological functions of GPR84. |
| WOS关键词 | PROTEIN-COUPLED-RECEPTOR ; FATTY-ACID RECEPTORS ; EXPRESSION |
| 资助项目 | National Natural Science Foundation of China[81425024] ; Ministry of Science and Technology of China[2015CB964503] ; Ministry of Science and Technology of China[2014CB541906] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000377845200009 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276018]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Xie, Xin; Nan, Fa-Jun |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, 189 Guoshoujing Rd, Shanghai 201203, Peoples R China; 2.E China Normal Univ, Dept Chem, 3663 North Zhong Shan Rd, Shanghai 200062, Peoples R China; 3.E China Normal Univ, Inst Med Chem, 3663 North Zhong Shan Rd, Shanghai 200062, Peoples R China; 4.Tongji Univ, Sch Life Sci & Technol, Shanghai Key Lab Signaling & Dis Res, Lab Receptor Based BioMed, 1239 Siping Rd, Shanghai 200092, Peoples R China; 5.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, 189 Guoshoujing Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Yang,Zhang, Qing,Chen, Lin-Hai,et al. Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists[J]. ACS MEDICINAL CHEMISTRY LETTERS,2016,7(6):579-583. |
| APA | Liu, Yang.,Zhang, Qing.,Chen, Lin-Hai.,Yang, Hui.,Lu, Wei.,...&Nan, Fa-Jun.(2016).Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists.ACS MEDICINAL CHEMISTRY LETTERS,7(6),579-583. |
| MLA | Liu, Yang,et al."Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists".ACS MEDICINAL CHEMISTRY LETTERS 7.6(2016):579-583. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。