Imidazole is a five-membered aromatic heterocyclic compound that occurs naturally in a variety of products. Its structure has a unique feature with electron-rich characteristics that are useful for imidazole and derivatives because they readily associate with enzymes and receptors in biological systems and have a wider range of bioactivities. Various imidazole derivatives are used in clinical practice to treat a variety of diseases with high therapeutic potency. This analysis covers the synthesis of imidazolebased derivatives and their applications as antibacterial, anticancer, antihypertensive, antimalarial, antifungal, antioxidant, antiviral, and analgesic agents, as well as their function in HIV-1 inhibitors, Alzheimer’s disease treatment, and Chagas disease treatment.