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Click chemistry, a powerful tool for pharmaceutical sciences

Journal

PHARMACEUTICAL RESEARCH
Volume 25, Issue 10, Pages 2216-2230

Publisher

SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-008-9616-1

Keywords

bioconjugation; click chemistry; drug delivery; nanomedicine; polymer

Funding

  1. NIH [AR053325]
  2. College of Pharmacy, University of Nebraska Medical Center
  3. NATIONAL INSTITUTE OF ARTHRITIS AND MUSCULOSKELETAL AND SKIN DISEASES [R01AR053325] Funding Source: NIH RePORTER

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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.

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