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1,2,3-triazole is a five-member nitrogen-containing heterocyclic compound with diverse biological activities. A number of 1,2,3-triazole-containing FDA-approved drugs are available on the market, and many other pharmaceutically significant potential molecules are under clinical investigation. Therefore, it is fairly reasonable to anticipate that there will be an increase in demand for new triazole-containing drugs in the coming future. Because of its broad pharmacological applications, it has recently attracted the attention of scientists worldwide. This review provides a concise summary of the synthetic techniques for triazole compounds from various strategies and their medical importance as a lead structure for the enhancement of therapeutic molecules.