Thiazolotriazoles: Their Biological Activity and Structure–Activity Relationships

Thiazolotriazole is gaining attention in medicinal chemistry due to its wide spectrum of biological activity. It is a fused heterocyclic compound formed by the fusion of 1,3-thiazole and 1,2,4-triazole, and the type of ring fusion results in the formation of isomeric thiazolotriazoles-[3,2-b] or [2,3-c] isomers. The synthesis of both ring systems has been carried out by various methodologies ranging from conventional methods such as cyclization and annulation to the use of metal catalysts, microwave radiation, photochemical and multicomponent reactions. In drug discovery, thiazolotriazole derivatives have been primarily investigated for their antibacterial, anticancer, anti-inflammatory, and antifungal properties. Recent years have seen significant advancements in anticancer drug research, revealing that these molecules are potential anticancer agents interacting with specific targets or biochemical pathways responsible for apoptosis and proliferation. In addition, thiazolotriazole also exhibits analgesic, anticonvulsant, antidiabetic, and antioxidant activities. Furthermore, thiazolotriazoles have also demonstrated the potential to inhibit enzymes such as carbonic anhydrase, urease, cyclooxygenase, and butyrylcholinesterase, which are meant to have particular biological functions. In the context of various applications, a review that describes biological activities with a particular focus on structural attributes that contribute to the activity will be helpful to better understand structure-activity relationship (SAR) and guide for further design of bioactive thiazolotriazoles. This review explains the biological activity of thiazolotriazole highlighting SAR and drug targets for specific disease conditions which will be helpful to better understand the scaffold and apply this knowledge to future drug discovery on thiazolotriazoles.