Click chemistry, a powerful tool for pharmaceutical sciences

Pharm Res. 2008 Oct;25(10):2216-30. doi: 10.1007/s11095-008-9616-1. Epub 2008 May 29.

Abstract

Click chemistry refers to a group of reactions that are fast, simple to use, easy to purify, versatile, regiospecific, and give high product yields. While there are a number of reactions that fulfill the criteria, the Huisgen 1,3-dipolar cycloaddition of azides and terminal alkynes has emerged as the frontrunner. It has found applications in a wide variety of research areas, including materials sciences, polymer chemistry, and pharmaceutical sciences. In this manuscript, important aspects of the Huisgen cycloaddition will be reviewed, along with some of its many pharmaceutical applications. Bioconjugation, nanoparticle surface modification, and pharmaceutical-related polymer chemistry will all be covered. Limitations of the reaction will also be discussed.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Alkynes / chemical synthesis*
  • Azides / chemical synthesis*
  • Catalysis
  • Chemistry, Pharmaceutical*
  • Copper / chemistry
  • Cyclization
  • Drug Carriers*
  • Liposomes
  • Metal Nanoparticles
  • Micelles
  • Models, Chemical
  • Molecular Probes / chemical synthesis*
  • Polymers / chemical synthesis*
  • Technology, Pharmaceutical / methods*

Substances

  • Alkynes
  • Azides
  • Drug Carriers
  • Liposomes
  • Micelles
  • Molecular Probes
  • Polymers
  • Copper