Recent advances in triazole synthesis via click chemistry and their pharmacological applications: A review

[Display omitted] Click chemistry is a flexible method featuring only the most feasible and efficient chemical reactions. The synthesis of 1,2,3-triazole from azides and terminal acetylenes using copper(I) as a catalyst is an extremely powerful reaction due to the extreme dependability, good selectivity, and biocompatibility of the starting materials. Triazole molecules are more than simple passive linkers; through hydrogen bonding and dipole interactions, they rapidly bind with biological targets. Its applications in drug development are expanding, ranging from target-oriented in situ chemistry and combinatorial mechanisms for lead generation to bioconjugation methods to study proteins and DNA. The click chemistry has frequently been used to speed up drug discovery and optimization processes in the past few years. The click chemistry reaction based on copper-catalyzed azide-alkyne cycloaddition (CuAAC) is a biochemical process with applications in medicinal chemistry and chemical biology. Thus, click reactions are an essential component of the toolkit for medicinal chemistry and help medicinal chemists overcome the barriers in chemical reactions, increase throughput, and improve the standards of compound libraries. The review highlights the recent advancements in the copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry approach for synthesizing biologically important triazole moieties with a greater emphasis on synthesis methodologies and pharmacological applications. Additionally, the triazole-based FDA-approved drugs are also discussed with their mode of action to highlight the importance of the click chemistry approach in synthesizing the bioactive triazole compounds.