The imidazole, benzimidazole, benzoxazole, tetrazole and quinazolinone are heterocyclic aromatic organic compounds. It is an important pharmacophore and privileged structure in medicinal chemistry. It plays a very important role with plenty of useful therapeutic activities such as antiulcers, antihypertensives, analgesic, antiinflammatory, anti-virals, antifungals, anticancer, antidepressant activity, antilishmanial activity, anticonvulsant activity, antitubercular activity, antitumor activity, cyclooxygenase-2 inhibiting activity, DNA Topoisomerase inhibiting activity, antileukemic activity, antimalarial activity, antioxidant activity, antileishmanial activity and antihistaminics. The review of the literature shows that the imidazole, benzimidazole, benzoxazole, tetrazole and quinazolinones derivatives are outstandingly effective compounds and a large number of reviews available for biochemical and pharmacological studies conformed that their molecules are useful against a wide variety of microorganisms. Because of their importance, the methods for their synthesis have become a focus of synthetic organic chemists. Therefore in the present review we tried to compile the chemistry of different derivative of substituted imidazole, benzimidazole, benzoxazole, tetrazole and quinazolinones as well as various pharmacological activities and some of the important methodologies used for the synthesis.