At the heart of current research is the battle for more efficient and less toxic treatment approaches for diseases. Pyrazole and its derivatives have emerged as an influential scaffold that has drawn the attention of researchers in the field of medicinal chemistry due to its appreciable diversity in biological activities. Pyrazole derivatives have found numerous applications in fluorescent substances, dyes, and agrochemicals. Pyrazole is a multifunction lead compound for efficient biologically active molecules generated by researchers. They have shown a widespread biological and pharmacological activity such as antitumor, analgesic, antiinflammatory, antimicrobial, antitubercular, antileishmanial activity, ACE inhibitors, antidiabetic, antiparkinsonian and neuroprotective properties. This rational diversity in the pattern of physiological reaction has led many scientists, with far more successful pharmacological intervention, to refine and create new structural alternatives. This Review is important for previous studies and initiatives to explore in the near future the various activities of compounds associated with pyrazole and pyrazole derivatives.