Lead compound optimization strategy (6)-improving the plasma stability
10.16438/j.0513-4870.2017-0934
- VernacularTitle:先导化合物结构优化策略(六)——改善化合物血浆稳定性
- Author:
Xiao-wei WU
1
;
Jiang WANG
1
;
Hong LIU
1
Author Information
1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
- Publication Type:REVIEWS
- Keywords:
plasma stability;
structural modification;
lead compound;
bioisosterism
- From:
Acta Pharmaceutica Sinica
2018;53(2):192-201
- CountryChina
- Language:Chinese
-
Abstract:
Plasma stability plays an important role in the druggability of lead compound. Improving the plasma stability of compounds by structural modification can lead to good pharmacokinetic and pharmacodynamics properties. This review provides a summary of varieties of structure modification strategies for improving plasma stability including bioisosterism, increasing steric hindrance, ring closure, scaffold hopping and etc.