Triazole has occur as a valuable platform in medicinal chemistry, acquiring assorted pharmacological properties, which could play a major role against the common mechanisms associated with various disorders like cancer, infections, inflammation, convulsions, oxidative stress and neurodegeneration etc. Structural modification of this scaffold could be helpful in the generation of new therapeutically useful agents. Although research endeavors are moving towards the growth of synthetic analogs of triazole, there is still lot of scope to achieve drug discovery break-through in this area. Upcoming therapeutic prospective of this moiety has apprehended the attention of medicinal chemists to synthesize novel triazole derivatives. Authors have amalgamated the chemistry, synthetic strategies and detailed pharmacological activities of this nucleus in the present review. Information regarding the marketed triazole derivatives has also been incorporated. The objective of the review is to endow with the insights to not only the synthetic but also to the medicinal chemists so as to design and synthesize the novel triazole derivatives with advanced and unexplored pharmacological implications.