title: Discovery of novel anti-HIV agents via Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry-based approach.
abstract: BACKGROUND
  In recent years, a variety of new synthetic methodologies and concepts have been proposed in the search for new pharmaceutical lead structures and optimization. Notably, the Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry approach has drawn great attention and has become a powerful tool for the generation of privileged medicinal skeletons in the discovery of anti-HIV agents. This is due to the high degree of reliability, complete specificity (chemoselectivity and regioselectivity), mild conditions, and the biocompatibility of the reactants.
  
  
  METHODS
  Herein, the authors describe the progress thus far on the discovery of novel anti-HIV agents via the CuAAC click chemistry-based approach.
  
  
  CONCLUSIONS
  CuAAC click chemistry is a proven protocol for synthesizing triazole products which could serve as basic pharmacophores, act as replacements of traditional scaffold or substituent modification, be a linker of dual-target or dual-site inhibitors and more for the discovery of novel anti-HIV agents. What's more, it also provides convenience and feasibility for dynamic combinatorial chemistry and in situ screening. It is envisioned that click chemistry will draw more attention and make more contributions in anti-HIV drug discovery in the future.
authors.affiliation: a Department of Medicinal Chemistry, Key laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , Jinan , P. R. China.
authors.forename: Ping
authors.initials: P
authors.lastname: Gao
authors.affiliation: a Department of Medicinal Chemistry, Key laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , Jinan , P. R. China.
authors.forename: Lin
authors.initials: L
authors.lastname: Sun
authors.affiliation: a Department of Medicinal Chemistry, Key laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , Jinan , P. R. China.
authors.forename: Junsu
authors.initials: J
authors.lastname: Zhou
authors.affiliation: a Department of Medicinal Chemistry, Key laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , Jinan , P. R. China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Li
authors.affiliation: a Department of Medicinal Chemistry, Key laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , Jinan , P. R. China.
authors.forename: Peng
authors.initials: P
authors.lastname: Zhan
authors.affiliation: a Department of Medicinal Chemistry, Key laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , Jinan , P. R. China.
authors.forename: Xinyong
authors.initials: X
authors.lastname: Liu
mesh_terms: D000480:Alkynes / Q000737:chemistry; D019380:Anti-HIV Agents / Q000737:chemistry*; D001386:Azides / Q000737:chemistry; D057930:Click Chemistry / Q000379:methods*; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D003300:Copper / Q000737:chemistry; D061565:Cycloaddition Reaction; D055808:Drug Discovery / Q000379:methods*; D015658:HIV Infections / Q000188:drug therapy
chemical_list: D000480:Alkynes; D019380:Anti-HIV Agents; D001386:Azides; D003300:Copper
keywords: CuAAC; HIV inhibitors; click chemistry; drug design; triazole