Click Chemistry: an overview and recent updates in the medicinal attributes of click-derived heterocycles

Recently, it has been seen that there is a rapid surge in Click Chemistry (CC) research owing to its fast, reliable, and biocompatible nature, making it an ideal tool for drug discovery. CC approach allows facile and sustainable development of complex molecules with minimal off-target products. With the rapid advancement of the CC field, its applications have significantly expanded across various domains, including biomedical, pharmaceutical, radiochemistry, nanochemistry, polymer chemistry, and microscopy. However, its applications remain most prominent in medicinal chemistry. This review initially covers the introduction and distinct types of click reactions such as copper-catalyzed azide-alkyne cycloaddition (CuAAC), strain-promoted azide-alkyne cycloaddition (SPAAC), and Diels–Alder Cycloaddition (DA), followed by the different techniques facilitating the click reactions. Among these, the CuAAC reaction is most effective and extensive CC approach widely explored for creating huge number of molecular libraries of medicinal significance due to its excellent biocompatibility, reliability, and specificity. In this review, we mainly included the synthesis and medicinal attributes of click reaction (CuAAC & SPAAC)-derived organic heterocycles from 2012–2023, particularly anticancer, antiviral, antidiabetic, and antimicrobial that will help the readers to understand the concept of CC, medicinal significance of CC-derived heterocycles, unexplored areas, challenges, and future prospects. This review will also provide a roadmap for new research directions and applications of click-derived heterocycles in medicinal chemistry.