Synthesis and PTP1B Inhibitory Activity of Novel Chalcone Derivatives Bearing 1H-Benzo[d]imidazol or 1H-Benzo[d][1,2,3]triazol Moieties
文献类型：期刊论文
| 作者 | Fu Yang1,3; Sheng Li2; Gao Lixin2; Li Jia2 ; Sun Liangpeng1
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| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
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| 出版日期 | 2019-04-01 |
| 卷号 | 39期号:4页码:1029-1036 |
| 关键词 | PTP1B inhibitor 1H-benzo[d]imidazol 1H-benzo[d][1,2,3]triazol chalcone |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201811030 |
| 通讯作者 | Li Jia(lpsun@ybu.edu.cn) ; Sun Liangpeng(jli@simm.ac.cn) |
| 英文摘要 | Protein tyrosine phosphatase 1B (PTP1B) inhibitor has recently been identified as new candidate drug for type II diabetes and obesity due to 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 chalcone derivatives bearing 1H-benzo[d]imidazol or 1H-benzo[d][1,2,3]triazol moieties were designed, synthesized, and evaluated for their PTP1B inhibitory activities. The results demonstrated that all compounds presented potent inhibitory activities against PTP1B, among which 2-(1H-benzo[d][1,2,3]triazol-1-yl)-N'-(4-(3-(naphthalen-2-yl)-3-oxoprop-1-en-1-yl) benzylidene) acetohydrazide (10i) exhibited the best potency with IC50 value of (2.98 +/- 0.04) mu mol.L-1. Importantly, 2-(1H-benzo[d][1,2,3] triazol-1-yl)-N'-(4-(3-oxo-3-(p-tolyl) prop-1-en-1-yl)benzylidene)acetohydrazide (10h) showed no significant inhibition on T-cell protein tyrosine phosphatase (TCPTP) at the concentration of 20 mu g/mL, suggesting the highly selectivity of this agent toward PTP1B. |
| WOS关键词 | TYROSINE-PHOSPHATASE 1B ; POTENT ; DISCOVERY ; ACID ; DESIGN |
| 资助项目 | National Natural Science Foundation of China[81460524] ; National Natural Science Foundation of China[81773779] ; Scientific Research Fund Project of Education Department of Jilin Province[2015-50] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000466156500012 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/289834]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Li Jia; Sun Liangpeng |
| 作者单位 | 1.Yanbian Univ, Med Coll, Yanji 133002, Peoples R China 2.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Changchun Inst Appl Chem, Changchun 130000, Jilin, Peoples R China |
| 推荐引用方式 GB/T 7714 | Fu Yang,Sheng Li,Gao Lixin,et al. Synthesis and PTP1B Inhibitory Activity of Novel Chalcone Derivatives Bearing 1H-Benzo[d]imidazol or 1H-Benzo[d][1,2,3]triazol Moieties[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2019,39(4):1029-1036. |
| APA | Fu Yang,Sheng Li,Gao Lixin,Li Jia,&Sun Liangpeng.(2019).Synthesis and PTP1B Inhibitory Activity of Novel Chalcone Derivatives Bearing 1H-Benzo[d]imidazol or 1H-Benzo[d][1,2,3]triazol Moieties.CHINESE JOURNAL OF ORGANIC CHEMISTRY,39(4),1029-1036. |
| MLA | Fu Yang,et al."Synthesis and PTP1B Inhibitory Activity of Novel Chalcone Derivatives Bearing 1H-Benzo[d]imidazol or 1H-Benzo[d][1,2,3]triazol Moieties".CHINESE JOURNAL OF ORGANIC CHEMISTRY 39.4(2019):1029-1036. |
入库方式： OAI收割
来源：上海药物研究所
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