Imidazole is a planar five- member heterocyclic ring with 3C and 5N atom with N atom present at the 1^st and 3^rd positions of the ring. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine and nucleic acid. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. The high therapeutic properties of the imidazole related drugs have encouraged the medicinal chemists to synthesize a large number of novel chemotherapeutic agents. Imidazole is an entity which explores different types of pharmacological and biological activities like metronidazole and nitrosoimidazole as bactericidal, 1­vinylimidazole as fungicidal, megazol as trypanocidal, imidazole­2­one as antileishmanial and other antimicrobial activities. This article aims to review the process of synthesis of imidazole and its derivatives by different methods and pharmacological activities