Chromone-Linked 1,2,3-Triazoles as Potent Molecules for Therapeutic Use

Abstract: Nitrogen-containing heterocycles have long been recognized for their structural diversity and biological significance, making them key targets for research. These compounds occur in particular naturally derived products and exhibit substantial chemical and biological relevance. In organic chemistry, they are essential and often possess therapeutic and pharmacological properties. The ability of heterocycles containing nitrogen and oxygen to influence physicochemical properties has led to the development of chromone-fused or embedded 1,2,3-triazoles, which have become highly significant in both medical and chemical research over recent decades. Medicinal chemists have found that combining two or more pharmacophores into well-known, biologically active compounds often enhances their performance. This strategy may yield complementary biological effects and enhance the efficacy of the parent molecules. The 1,2,3-triazole moiety is a crucial pharmacophore in this class of heterocycles, and its potential for developing more potent agents with enhanced activity is highly promising. To explore novel chemical landscapes for drug-like compounds with greater structural diversity, integrating diversityoriented synthesis with 'privileged' motifs and bioorthogonal reactions, alongside advanced automation and flow technologies, could improve efficiency in drug discovery. This review highlights the role of 1,2,3- triazoles, synthesized via click chemistry, in exhibiting antimicrobial, antitubercular, antidiabetic, anticancer, anticholinesterase, and anticonvulsant activities. It also examines chromone-based 1,2,3-triazoles, which have garnered considerable attention from 2008 to 2025 due to their broad antimicrobial and anticancer potential.