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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:1092  下载量:511
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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