Organic Chemistry Division, National Chemical Laboratory, Dr. Homi Bhabha Road, Pashan, Pune, India.
Chem Asian J. 2011 Oct 4;6(10):2696-718. doi: 10.1002/asia.201100432. Epub 2011 Aug 29.
The copper(I)-catalyzed 1,2,3-triazole-forming reaction between azides and terminal alkynes has become the gold standard of 'click chemistry' due to its reliability, specificity, and biocompatibility. Applications of click chemistry are increasingly found in all aspects of drug discovery; they range from lead finding through combinatorial chemistry and target-templated in vitro chemistry, to proteomics and DNA research by using bioconjugation reactions. The triazole products are more than just passive linkers; they readily associate with biological targets, through hydrogen-bonding and dipole interactions. The present review will focus mainly on the recent literature for applications of this reaction in the field of medicinal chemistry, in particular on use of the 1,2,3-triazole moiety as pharmacophore.
铜（I）催化的叠氮化物和末端炔烃之间的 1,2,3-三唑形成反应由于其可靠性、特异性和生物相容性已成为“点击化学”的黄金标准。点击化学的应用在药物发现的各个方面都越来越多；它们从通过组合化学和靶标导向的体外化学发现先导化合物，到使用生物缀合反应的蛋白质组学和 DNA 研究。三唑产物不仅仅是被动连接子；它们通过氢键和偶极相互作用很容易与生物靶标结合。本综述将主要关注该反应在药物化学领域的最新文献，特别是将 1,2,3-三唑部分用作药效团。
