Click Chemistry: 1,2,3-Triazoles as Pharmacophores

被引：1180

作者：

Agalave, Sandip G. ^{[1
]}

Maujan, Suleman R. ^{[1
]}

Pore, Vandana S. ^{[1
]}

机构：

[1] Natl Chem Lab, Div Organ Chem, Pune, Maharashtra, India

来源：

CHEMISTRY-AN ASIAN JOURNAL | 2011年 / 6卷 / 10期

关键词：

click chemistry; copper; cycloaddition; pharmacophores; triazoles; AZIDE-ALKYNE CYCLOADDITION; ONE-POT SYNTHESIS; BIOLOGICAL EVALUATION; 1,3-DIPOLAR CYCLOADDITION; SELECTIVE INHIBITORS; ANTIMICROBIAL ACTIVITY; RECEPTOR ANTAGONISTS; SIDEROPHORE BIOSYNTHESIS; ANTIBACTERIAL ACTIVITY; PARALLEL SYNTHESIS;

D O I：

10.1002/asia.201100432

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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.

引用

页码：2696 / 2718

页数：23

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