Comprehensive review on natural pharmacophore tethered 1,2,3‐triazoles as active pharmaceuticals

Abstract The privileged 1,2,3‐triazole scaffold is drawing researcher's attention due to its widespread applications in diverse fields such as drug discovery (e.g., carboxyamidotriazole), organic synthesis (click‐reaction template), polymeric materials (e.g., triazolamer), supramolecular receptors (e.g., triazolophane), fluorescent materials (e.g., metal–organic frameworks), and agricultural sectors (e.g., fungicides). Various 1,2,3‐triazole persuasion modules are also currently available in the market that have multiple assets such as active pharmaceuticals and agricultural purposes. Owed to the highly consistent and firmest synthesis approach, that is, click reaction of various azides and acetylene derivatives by copper (I)‐catalyzed 1,3‐dipolar cycloaddition (CuAAC), highly functionalized 1,2,3‐triazoles are prepared in scalar yields for drug discovery. Given the importance of 1,2,3‐triazole chemistry, the present review focuses specifically on the synthesis of structurally diverse 1,2,3‐triazoles linked to natural pharmacophores and their biological importance. Furthermore, the dual/multi‐pharmacophores assimilated 1,2,3‐triazoles have listed interesting biological activities that could be valuable as future drug leads. In addition, this comprehensive review can serve as a template for the development of new diverse scaffolds that will ensure for new therapeutic approaches for the existing myriad diseases and disorders.