Li Zeng, Wang Jiang, Zhou Yu, Liu Hong
Yao Xue Xue Bao. 2014 Sep;49(9):1238-47.
Water solubility is an essential physical chemistry property of organic small molecule drug and is also a very important issue in drug discovery. Good water solubility often leads to a good drug potency and pleasant pharmacokinetic profiles. To improve water solubility, structure modification is a straight and effective way based on the theory of water solubility. This review summarized valid structure modification strategies for improving water solubility including salt formation, polar group introduction, liposolubility reduction, conformation optimization and prodrug.
水溶性是有机小分子药物的一项基本物理化学性质，也是药物研发中一个非常重要的问题。良好的水溶性通常会带来良好的药物效力和令人满意的药代动力学特征。基于水溶性理论，结构修饰是提高水溶性直接且有效的方法。本文综述了提高水溶性的有效结构修饰策略，包括成盐、引入极性基团、降低脂溶性、构象优化和前药。
