Synthesis and PTP1B Inhibitory Activity of (E)-1-Substitutedphenyl-3-(4-((E)-(2-(4-phenylthiazol-2-yl)hydrazono)methyl)pheny1)-prop-2-en-1-ones
文献类型：期刊论文
| 作者 | Sun Liangpeng3; Jiang Zhe1; Gao Lixin2; Liu Xiaofang3; Quan Yingchun3; Zheng Guanghao3; Li Jia2 ; Piao Huri3
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2013-07 |
| 卷号 | 33期号:7页码:1496-1502 |
| 关键词 | PTP1B inhibitor chalcone carboxaldehyde hydrazone thiazole |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201212012 |
| 文献子类 | Article |
| 英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) has recently been identified as new drug target for type II diabetes and obesity due to that it is a negative regulator of the insulin and leptin-signaling pathway. In order to find new nonphosphonate-based pTyr mimetics, a series of novel (E)-1-phenyl-3-(44(E)-(2-(4-phenyl-thiazol-2-yl)hydrazono)methyl)phenyl)-prop-2-en-1-one (4a similar to 4n) were designed, synthesized, and evaluated for their PTP1B inhibitory activity. The results demonstrated that all compounds presented potent inhibitory activities against PTP1B, among which compound 4h exhibited most potent with IC50 value of (2.57 +/- 0.50) mu mol-L-1. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; STRUCTURE-BASED DESIGN ; CHALCONE DERIVATIVES ; ANTIBACTERIAL ; SPECIFICITY ; HYDRAZONES ; DISCOVERY ; MOIETY ; POTENT ; AGENTS |
| 资助项目 | National Natural Science Foundation of China[81160381] ; National Natural Science Foundation of China[81125023] |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:4908608 |
| WOS记录号 | WOS:000323797100015 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277544]  |
| 专题 | 国家新药筛选中心 药物安全性评价中心 |
| 通讯作者 | Sun Liangpeng |
| 作者单位 | 1.Yanbian Univ Hosp, Yanji 133002, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 3.Yanbian Univ, Coll Pharm, Minist Educ, Key Lab Nat Resources Changbai Mt & Funct Mol, Yanji 133002, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Sun Liangpeng,Jiang Zhe,Gao Lixin,et al. Synthesis and PTP1B Inhibitory Activity of (E)-1-Substitutedphenyl-3-(4-((E)-(2-(4-phenylthiazol-2-yl)hydrazono)methyl)pheny1)-prop-2-en-1-ones[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2013,33(7):1496-1502. |
| APA | Sun Liangpeng.,Jiang Zhe.,Gao Lixin.,Liu Xiaofang.,Quan Yingchun.,...&Piao Huri.(2013).Synthesis and PTP1B Inhibitory Activity of (E)-1-Substitutedphenyl-3-(4-((E)-(2-(4-phenylthiazol-2-yl)hydrazono)methyl)pheny1)-prop-2-en-1-ones.CHINESE JOURNAL OF ORGANIC CHEMISTRY,33(7),1496-1502. |
| MLA | Sun Liangpeng,et al."Synthesis and PTP1B Inhibitory Activity of (E)-1-Substitutedphenyl-3-(4-((E)-(2-(4-phenylthiazol-2-yl)hydrazono)methyl)pheny1)-prop-2-en-1-ones".CHINESE JOURNAL OF ORGANIC CHEMISTRY 33.7(2013):1496-1502. |
入库方式： OAI收割
来源：上海药物研究所
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