1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

Bioorg Med Chem. 2019 Aug 15;27(16):3511-3531. doi: 10.1016/j.bmc.2019.07.005. Epub 2019 Jul 4.

Abstract

The 1,2,3-triazole ring is a major pharmacophore system among nitrogen-containing heterocycles. These five-membered heterocyclic motifs with three nitrogen heteroatoms can be prepared easily using 'click' chemistry with copper- or ruthenium-catalysed azide-alkyne cycloaddition reactions. Recently, the 'linker' property of 1,2,3-triazoles was demonstrated, and a novel class of 1,2,3-triazole-containing hybrids and conjugates was synthesised and evaluated as lead compounds for diverse biological targets. These lead compounds have been demonstrated as anticancer, antimicrobial, anti-tubercular, antiviral, antidiabetic, antimalarial, anti-leishmanial, and neuroprotective agents. The present review summarises advances in lead compounds of 1,2,3-triazole-containing hybrids, conjugates, and their related heterocycles in medicinal chemistry published in 2018. This review will be useful to scientists in research fields of organic synthesis, medicinal chemistry, phytochemistry, and pharmacology.

Keywords: 1,2,3-Triazole; Biological activity; Click chemistry; Copper-catalysed 1,3-dipolar cycloaddition (CuAAC); Huisgen azide-alkyne cycloaddition; Lead compounds.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Chemistry, Pharmaceutical / methods*
  • Triazoles / chemistry*

Substances

  • Triazoles