Lead compound optimization strategy (1)--changing metabolic pathways and optimizing metabolism stability.
- Author:
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:Journal Article
- MeSH:
Animals;
Biological Availability;
Drug Design;
Drug Discovery;
Drug Stability;
Half-Life;
Humans;
Metabolic Networks and Pathways;
Pharmaceutical Preparations;
chemical synthesis;
chemistry;
metabolism
- From:
Acta Pharmaceutica Sinica
2013;48(10):1521-1531
- CountryChina
- Language:Chinese
-
Abstract:
Lead compound optimization plays an important role in new drug discovery and development. The strategies for changing metabolic pathways can modulate pharmacokinetic properties, prolong the half life, improve metabolism stability and bioavailability of lead compounds. The strategies for changing metabolic pathways and improving metabolism stability are reviewed. These methods include blocking metabolic site, reduing lipophilicity, changing ring size, bioisosterism, and prodrug.
