| 氟原子在药物分子设计中的应用 |
| |
| 引用本文： | 王江,柳红. 氟原子在药物分子设计中的应用[J]. 有机化学, 2011, 31(11) |
| |
| 作者姓名： | 王江 柳红 |
| |
| 作者单位： | 中国科学院上海药物研究所新药研究国家重点实验室 上海201203 |
| |
| 摘 要： | 含氟药物在临床治疗药物中占有相当比重.将氟原子或含氟基团引入到小分子药物中,是药物化学结构改造的重要研究策略之一.综述了氟原子在药物分子设计中的应用,氟原子或含氟基团的引入可以调节药物小分子的物理化学特性,改变小分子的药代动力学性质,提高药物的生物利用度；通过影响化合物的构象,增强配体与靶标蛋白的相互结合能力以及对其它靶标蛋白的选择性；通过阻断易代谢位点进而提高药物代谢稳定性等.
|
| 关 键 词： | 氟 药物设计 结构优化 |
Application of Fluorine in Drug Design |
| |
| Wang, Jiang,Liu, Hong. Application of Fluorine in Drug Design[J]. Chinese Journal of Organic Chemistry, 2011, 31(11) |
| |
| Authors: | Wang Jiang Liu Hong |
| |
| Affiliation: | Wang,Jiang Liu,Hong (State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203) |
| |
| Abstract: | Fluorinated compounds comprise a substantial proportion in the therapeutic drugs.It is an important strategy to introduce fluorine and fluorinated substitutes in the small molecule for structure-based medicinal chemistry.They can modulate the physicochemical and pharmacokinetic properties to improve bioavailability,alter the conformation of a molecule to enhance the selectivities and binding affinity to target proteins,and block metabolically labile sites to increase the metabolic stability of drugs. |
| |
| Keywords: | fluorine drug design lead optimization |
| 本文献已被 CNKI 万方数据 等数据库收录！ |
|
