[Lead compound optimization strategy (1)--changing metabolic pathways and optimizing metabolism stability]

Jiang Wang; Hong Liu

[Lead compound optimization strategy (1)--changing metabolic pathways and optimizing metabolism stability]

Yao Xue Xue Bao. 2013 Oct;48(10):1521-31.

[Article in Chinese]

Authors

Jiang Wang¹, Hong Liu¹

Affiliation

¹ State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

PMID: 24417078

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.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Animals
Biological Availability
Drug Design*
Drug Discovery*
Drug Stability*
Half-Life
Humans
Metabolic Networks and Pathways*
Pharmaceutical Preparations / chemical synthesis
Pharmaceutical Preparations / chemistry
Pharmaceutical Preparations / metabolism*

Substances

Pharmaceutical Preparations