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药学学报  2014 

先导化合物结构优化策略(三)——通过化学修饰改善水溶性

, PP. 1238-1247

Keywords: 水溶性,结构修饰,前药,先导化合物优化

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Abstract:

水溶性是有机小分子药物极为重要的物理化学性质,也是小分子药物研发过程中的关键问题之一。良好的水溶性有助于药效的发挥和药代动力学性质的改善。在药物化学领域,通过化学结构修饰方法改善药物的水溶性,是从溶解的本质上考虑和解决问题的基本方法。本文综述了通过化学结构修饰改善水溶性的基本策略,包括成盐修饰、引入极性基团、降低脂溶性、构象优化、前药修饰等。

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