| Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice | |
| Jiang, Bo1,2; Guo, Shuju1,2; Shi, Dayong1,2; Guo, Chao1; Wang, Tao3; Shi, DY | |
| 2013-06-01 | |
| 发表期刊 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| ISSN | 0223-5234 |
| 卷号 | 64页码:129-136 |
| 文章类型 | Article |
| 摘要 | In an effort to develop novel small molecule PTP1B inhibitors, a series of bromophenol derivatives were designed, synthesized and evaluated in vitro and in vivo. All of the synthesized compounds displayed weak to potent PTP1B inhibitory activities (5.62-9625%) at 20 mu g/mL. Among these compounds, 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol (9) exhibited enhanced PTP1B inhibitory activity (IC50 = 1.50 mu M) than the lead compound BDDPM (IC50 = 2.42 mu M) and high selectivity against other PTPs (TCPTP, LAR, SHP-1 and SHP-2). Results of anti-diabetic assay using C57BL/KsJ-db/db mouse model demonstrated that compound 9 was effective at lowering blood glucose, total cholesterol and HbA1c (P < 0.01). (C) 2013 Elsevier Masson SAS. All rights reserved.; In an effort to develop novel small molecule PTP1B inhibitors, a series of bromophenol derivatives were designed, synthesized and evaluated in vitro and in vivo. All of the synthesized compounds displayed weak to potent PTP1B inhibitory activities (5.62-9625%) at 20 mu g/mL. Among these compounds, 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol (9) exhibited enhanced PTP1B inhibitory activity (IC50 = 1.50 mu M) than the lead compound BDDPM (IC50 = 2.42 mu M) and high selectivity against other PTPs (TCPTP, LAR, SHP-1 and SHP-2). Results of anti-diabetic assay using C57BL/KsJ-db/db mouse model demonstrated that compound 9 was effective at lowering blood glucose, total cholesterol and HbA1c (P < 0.01). (C) 2013 Elsevier Masson SAS. All rights reserved. |
| 关键词 | Type 2 Diabetes Mellitus Protein Tyrosine Phosphatase 1b Bromophenol Anti-diabetic Activities |
| 学科领域 | Pharmacology & Pharmacy |
| DOI | 10.1016/j.ejmech.2013.03.037 |
| URL | 查看原文 |
| 收录类别 | SCI ; IC |
| 语种 | 英语 |
| WOS研究方向 | Pharmacology & Pharmacy |
| WOS类目 | Chemistry, Medicinal |
| WOS记录号 | WOS:000321230300014 |
| WOS关键词 | INSULIN SENSITIVITY ; PTP1B ; OBESITY ; CANCER ; GLUCOSE ; TARGET |
| WOS标题词 | Science & Technology ; Life Sciences & Biomedicine |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.qdio.ac.cn/handle/337002/16695 |
| 专题 | 海洋生物技术研发中心 |
| 通讯作者 | Shi, DY |
| 作者单位 | 1.Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China 2.Chinese Acad Sci, Inst Oceanol, Nantong Branch, Nantong 226006, Peoples R China 3.China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210009, Peoples R China |
| 第一作者单位 | 中国科学院海洋研究所 |
| 推荐引用方式 GB/T 7714 | Jiang, Bo,Guo, Shuju,Shi, Dayong,et al. Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2013,64:129-136. |
| APA | Jiang, Bo,Guo, Shuju,Shi, Dayong,Guo, Chao,Wang, Tao,&Shi, DY.(2013).Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,64,129-136. |
| MLA | Jiang, Bo,et al."Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 64(2013):129-136. |
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