The Use of Click Chemisty in Drug Development Applications

Click chemistry is defined as powerful, reliable, and selective reactions that assemble small building blocks via heteroatom linkages. Click reactions are a modular strategy that is a practical and convenient approach to chemical transformations. This strategy has been a promising approach for challenging processes such as mild reaction conditions, easy purification of intermediates, and imaging of drug targets. These advantages have added a new dimension to drug discovery and development in pharmaceutical sciences. Click reactions are interesting reactions that are currently studied in drug development studies, bioconjugation, polymer and material chemistry, and drug delivery systems. In this review, important highlights of the copper-catalyzed Huisgen 1,3-dipolar cycloaddition reaction, which is recognized to be the gold standard of click chemistry because of its biocompatibility and reliability, and the use of the selectively formed 1,2,3-triazole in drug development studies are discussed.