Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement
文献类型：期刊论文
| 作者 | Zhang, Mei2,3,4 ; Yang, Xiao-Ying5; Tang, Wei5; Groeneveld, Tom W. L.1; He, Pei-Lan5; Zhu, Feng-Hua5; Li, Jia4; Lu, Wei2,3; Blom, Anna M.1; Zuo, Jian-Ping5
|
| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2012-04 |
| 卷号 | 3期号:4页码:317-321 |
| 关键词 | high-throughput screening structural modification complement inhibitors C9 |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/ml300005w |
| 文献子类 | Article |
| 英文摘要 | A series of 1-phenyl-3-(1-phenylethyl)urea derivatives were identified as novel and potent complement inhibitors through structural modification of the original compound from high-throughput screening. Various analogues (7 and 13-15) were synthesized and identified as complement inhibitors, with the introduction of a five- or six-carbon chain (7c, 7d, 7k, 7I, and 7o) greatly improving their activity. Optimized compound 7I has an excellent inhibition activity with IC50 values as low as 13 nM. We demonstrated that the compound 7I inhibited C9 deposition through the classical, the lectin, and the alternative pathways but had no influence on C3 and C4 depositions. |
| WOS关键词 | MODIFIED CURTIUS REACTION ; CONVENIENT REAGENT |
| 资助项目 | National Natural Science Foundation of China[30725049] ; National Natural Science Foundation of China[81021062] ; National Natural Science Foundation of China[81072652] ; Shanghai Science and Technology Committee[11431921102] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000302591000012 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278131]  |
| 专题 | 药理学第一研究室 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 国家新药筛选中心 |
| 通讯作者 | Blom, Anna M. |
| 作者单位 | 1.Lund Univ, Dept Lab Med, Sect Med Prot Chem, S-20502 Malmo, Sweden; 2.E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China; 3.E China Normal Univ, Inst Med Chem, Shanghai 200062, Peoples R China; 4.Chinese Acad Sci, Chinese Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 5.Chinese Acad Sci, Lab Immunopharmacol, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Mei,Yang, Xiao-Ying,Tang, Wei,et al. Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement[J]. ACS MEDICINAL CHEMISTRY LETTERS,2012,3(4):317-321. |
| APA | Zhang, Mei.,Yang, Xiao-Ying.,Tang, Wei.,Groeneveld, Tom W. L..,He, Pei-Lan.,...&Nan, Fa-Jun.(2012).Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement.ACS MEDICINAL CHEMISTRY LETTERS,3(4),317-321. |
| MLA | Zhang, Mei,et al."Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement".ACS MEDICINAL CHEMISTRY LETTERS 3.4(2012):317-321. |
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。