title: The impact of click chemistry in medicinal chemistry.
abstract: BACKGROUND
  The copper(I)-catalyzed 1,3-dipolar cycloaddition of alkynes and azides to form 1,2,3-triazoles is the most popular reaction in click chemistry. This reaction is also near-perfect, in terms of its robustness, due to the high degree of reliability and complete specificity. Furthermore, this reaction has been used increasingly in drug discovery, because the formed 1,2,3-triazole can act as both a bioisostere and a linker.
  
  
  METHODS
  This review provides an overview of a most important click reaction, 1,3-dipolar cycloadditions of alkynes and azides, in the drug discovery.
  
  
  CONCLUSIONS
  Click chemistry is a very powerful tool, in the drug discovery, because it is very efficient in the creation of compound libraries through combinatorial methodology. However, the 1,2,3-triazole ring itself is not a commonly used pharmacophore and has rarely been found in marketed drugs, demonstrating that there are still some limitations during the use of 1,2,3-triazole in the molecules of drug candidates. Hopefully, in the next decade, we will witness the emergence of 1,2,3-triazole-bearing drugs on the market as this click reaction is used more and more widely in the drug discovery.
authors.affiliation: Nankai University, State Key Laboratory of Medicinal Chemical Biology and College of Pharmacy, Tianjin 300071, PR China.
authors.forename: Jingli
authors.initials: J
authors.lastname: Hou
authors.forename: Xifang
authors.initials: X
authors.lastname: Liu
authors.forename: Jie
authors.initials: J
authors.lastname: Shen
authors.forename: Guilong
authors.initials: G
authors.lastname: Zhao
authors.forename: Peng George
authors.initials: PG
authors.lastname: Wang
mesh_terms: D000480:Alkynes / Q000737:chemistry; D001386:Azides / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D057930:Click Chemistry / Q000379:methods*; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*
chemical_list: D000480:Alkynes; D001386:Azides