Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor
文献类型：期刊论文
| 作者 | Han, Shuang1; Zhang, Fei-Fei2; Qian, Hai-Yan1; Chen, Li-Li1 ; Pu, Jian-Bin1; Xie, Xin2; Chen, Jian-Zhong1
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| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-08-13 |
| 卷号 | 58期号:15页码:5751-5769 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.5b00227 |
| 文献子类 | Article |
| 英文摘要 | The cannabinoid type 2 receptors (CB2Rs) play crucial roles in inflammatory diseases. There has been considerable interest in developing potent and selective ligands for CB2R. In this study, quinoline-2,4(1H,3H)-dione analogs have been designed, synthesized, and evaluated for their potencies and binding properties toward the cannabinoid type 1 receptor (CB1R) and CB2R C5- or C8-substituted quinoline-2,4(1H,3H)-diones demonstrate CB2R agonist activity, while the C6- or C7-substituted analogs are antagonists of CB2R In addition, oral administration of 21 dose-dependently alleviates the clinical symptoms of experimental autoimmune encephalomyelitis in a mouse model of multiple sclerosis and protects the central nervous system from immune damage. Furthermore, the interaction modes predicted by docking simulations and the 3D-QSAR model generated with CoMFA may offer guidance for further design and modification of CB2R modulators. |
| WOS关键词 | MOLECULAR-DYNAMICS SIMULATION ; HUMAN CB2 RECEPTOR ; MULTIPLE-SCLEROSIS ; PHARMACOLOGICAL CHARACTERIZATION ; ENDOCANNABINOID SYSTEM ; BIOLOGICAL EVALUATION ; CONTACT-DERMATITIS ; INVERSE AGONISTS ; IN-VITRO ; DISCOVERY |
| 资助项目 | National Natural Science Foundation of China[NSFC 30973637] ; Qanjiang Talents Project of Technology Office in Zhejiang Province[2010R10048] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | AMER CHEMICAL SOC |
| WOS记录号 | WOS:000359683700005 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276437]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Xie, Xin |
| 作者单位 | 1.Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Han, Shuang,Zhang, Fei-Fei,Qian, Hai-Yan,et al. Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor[J]. JOURNAL OF MEDICINAL CHEMISTRY,2015,58(15):5751-5769. |
| APA | Han, Shuang.,Zhang, Fei-Fei.,Qian, Hai-Yan.,Chen, Li-Li.,Pu, Jian-Bin.,...&Chen, Jian-Zhong.(2015).Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.JOURNAL OF MEDICINAL CHEMISTRY,58(15),5751-5769. |
| MLA | Han, Shuang,et al."Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor".JOURNAL OF MEDICINAL CHEMISTRY 58.15(2015):5751-5769. |
入库方式： OAI收割
来源：上海药物研究所
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