Imidazole is a compound that has been synthesized in a variety of its derivative forms over the past few years; the compound is a key source of interest to investigate its many pharmacological potentials. The chemistry of imidazole and its pharmacological effects as an antiviral, antimalarial, anticonvulsant, anticancer, antifungal, and anti-inflammatory medication are reviewed in this article by examining its different synthetic derivatives. Based to the available information, imidazole is a hetero-atomic planar five-member ring structure with a variety of chemical properties that can be utilized by generating derivatives with different pharmacological effects. In this article, the effects of various substitutions and combinations of various moieties with imidazole are discussed.