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新型PTP1B抑制剂的设计合成及生物活性研究
发表时间：2012-06-15 浏览量：1536 下载量：675
| 全部作者： | 童元峰，张裴，叶菲，吴松 |
| 作者单位： | 中国医学科学院北京协和医学院药物研究所，活性物质的发现与适药化研究北京市重点实验室；中国医学科学院北京协和医学院药物研究所 |
| 摘 要： | 目的：通过对先导物的结构优化获得一系列抑制蛋白酪氨酸磷酸酶- 1B（protein tyrosine phosphatase 1B，PTP1B）活性的化合物，期望发现新的糖尿病候选药物。方法：在前期以N- (2- 十四烷氧基苯基)邻氨甲酰基苯甲酸为先导物的基础上，设计合成一系列衍生物，并进行PTP1B活性筛选。结果：合成了13个目标化合物并测定了对PTP1B的活性。结论：体外活性测试结果显示，部分化合物的活性与先导物相当，其中一个化合物的IC50值达到100 nm左右。 |
| 关 键 词： | 药物化学；N- (2- 十四烷氧基苯基)邻氨甲酰基苯甲酸；先导物；合成；蛋白酪氨酸磷酸酶- 1B |
| Title： | Design, synthesis and bioactivity of novel PTP1B inhibitors |
| Author： | TONG Yuanfeng, ZHANG Pei, YE Fei, WU Song |
| Organization： | Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College; Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College |
| Abstract： | Objective: To find novel drug candidate for diabetes, a series of compounds against protein tyrosine phosphatase 1B (PTP1B) were found by the modification of the lead compound. Methods: Starting from N- (2- tetradecanoxyphenylaminocarbonyl) benzoic acid as lead compound, a series of derivatives were designed and synthesized. The inhibitory activities of these compounds in vitro against PTP1B were evaluated. Results: 13 compounds were synthesized and the activities were evaluated against PTP1B. Conclusion: The results indicated that some of the derivatives showed similar activities against PTP1B with the lead compound and IC50 of a compound arrived at 100 nm in vitro. |
| Key words： | medicinal chemistry; N- (2- tetradecanoxyphenylaminocarbonyl) benzoic acid; lead compound; synthesis; protein tyrosine phosphates 1B |
| 发表期数： | 2012年6月第11期 |
| 引用格式： | 童元峰，张裴，叶菲，等. 新型PTP1B抑制剂的设计合成及生物活性研究[J]. 中国科技论文在线精品论文，2012，5（11）：1018-1023. |
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