Over the last few decades, pyrazolone derivatives have been used for various biochemical applications. Some of these derivatives such as metamizole, phenazone, aminopyrine and propyphenazone, are widely used as antiinflammatory and analgesics. Moreover, pyrazolones have been exhibited antioxidant, antibacterial, anticancer and several other biological activities. Thus, keeping in view of their importance, synthetic strategies for existing as well as novel pyrazolone derivatives have been developed and explored their biochemical utility. As versatile features of pyrozaolones have emerged, so the aim of the present paper is to put chemical synthetic schemes and biological advancements of pyrazolone derivatives together.