Pyrazolines are five-membered heterocyclic compounds that play a significant role in drug discovery. Pyrazolines are promising bioactive scaffolds of great medicinal interest due to their diverse pharmacological and biological activities. The various activities associated with these moieties include antibacterial, antifungal, antitubercular, antioxidant, anti-inflammatory, anticancer, antihypertensive, analgesic, antiviral, anticonvulsant, sedative, and other significant pharmacological activities. The pyrazoline nucleus is often used to develop a number of new therapeutic agents. Hence, pyrazoline and its derivatives form an important class of heterocyclic compounds for new drug development.