| Summary: | Five-membered nitrogen heterocyclic compounds are a very important group with various pharmaceutical properties. The different substitutions and functionalization of these compounds contributed to various biological activities. Five-membered nitrogen heterocyclic scaffolds are used for synthesizing numerous natural and synthetic compounds with a significant biological application. They include antidiabetic, anticancer, antimalarial, antiviral, antimicrobial, anti-inflammatory, antibacterial, and anti-neurodegenerative agents. This mini-review provides an overview of the biological activities and the synthetic methods for preparing the five-membered nitrogen heterocyclic scaffolds and their functionalization. In the final part, this mini-review also listed some commercial drugs containing five-membered nitrogen heterocyclic motifs, highlighting the versatility of the five-membered nitrogen heterocyclic core in drug discovery. © 2022 The Japan Institute of Heterocyclic Chemistry.
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