点击化学
环加成
组合化学
药效团
化学
药物发现
叠氮化物
化学选择性
炔烃
计算机科学
纳米技术
有机化学
立体化学
材料科学
催化作用
生物化学
作者
Ping Gao,Lin Sun,Junsu Zhou,Li Xiao,Peng Zhan,Xinyong Liu
标识
DOI:10.1080/17460441.2016.1210125
摘要
Introduction: 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.Areas covered: Herein, the authors describe the progress thus far on the discovery of novel anti-HIV agents via the CuAAC click chemistry-based approach.Expert opinion: 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.
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