1,2,4-Triazole-containing scaffolds are unique heterocyclic compounds present in an array of pharmaceuticals and biologically important compounds used in the drug-discovery studies against cancer cells, microbes, and various types of disease in the human body. This review article summarizes the pharmacological significance of the 1,2,4-triazole-containing scaffolds and highlights the latest strategies for the synthesis of these privileged scaffolds using 3-amino-1,2,4-triazole. This review stimulates further research to find new and efficient methodologies for accessing new 1,2,4-triazole-containing scaffolds which would be very useful for the discover of new drug candidates.