Lead compound optimization strategy (3)--Structure modification strategies for improving water solubility.
- Author:
Zeng LI
;
Jiang WANG
;
Yu ZHOU
;
Hong LIU
- Publication Type:Journal Article
- MeSH:
Drug Design;
Prodrugs;
chemistry;
Solubility;
Structure-Activity Relationship;
Water;
chemistry
- From:
Acta Pharmaceutica Sinica
2014;49(9):1238-1247
- CountryChina
- Language:Chinese
-
Abstract:
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.
