OBJECTIVE: Imidazole is a heterocyclic moiety having immense biological importance. Since ancient times, the imidazole nucleus is considered to be a promising moiety in the field of chemistry. Preliminary in vitro and in vivo studies have provided valuable scientific evidence for its use. Subsequently, imidazole constitutes a new class of compounds for new drug development as the presence of this nucleus in diverse therapeutic categories viz; antimicrobial, anti-inflammatory, anticancer, immunomodulator, antiviral etc. has made it an interesting moiety for the design and development of new pharmacological agents. Thus, this review aims to summarize the reported molecular entities which were synthesized by using conventional as well as microwave processes, chemistry and biological potential of imidazole containing heterocyclic molecules while identifying potential areas of further research on imidazole. RESULTS: The review comprises literature pertaining to the evidence-based pharmacological or therapeutic potential of imidazole using published articles and worldwide databases. Various pharmacological experiments using different models exclusively proved the potential of imidazole. SUMMARY: Focusing on the discovery and development of new imidazole nucleus based molecules at a faster rate, there is a need to search previous information available in the market in the field of medicinal chemistry. Therefore, the present review aims to elaborate the therapeutic worth of imidazole and its analogs.