Advancements in Pyrazoline-Based Therapeutics: Synthesis, SAR and Pharmacological Outcomes (2021-2025)

Abstract

Pyrazolines are five-membered heterocyclic compounds containing three carbon atoms, two nitrogen atoms, and a single endocyclic bond. Because of their intriguing electrical characteristics and electron-rich nitrogen carriers, they have immense potential for dynamic pharmacological applications. It has gained the interest of many researchers and chemists, who have used this moiety in their research to design and synthesize new schemes and different derivatives. The objective of this review is to provide important information: a) to conclude Pyrazoline synthetic methods and marketed drugs; b) to summarize the synthesis, SAR, and biological action of potent compounds. The activities included in this review are anticancer, antitubercular, antimicrobial, antioxidant, and anti-inflammatory, along with a total of 30 schemes. A comprehensive literature search was conducted across major scientific databases, including ScienceDirect, PubMed, SciFinder, Google Scholar, and Crossref. Relevant studies published between 2021 and 2025 were systematically screened and analyzed, with data collected on the therapeutic potential of pyrazoline derivatives, encompassing synthesis methods, marketed formulations, SAR studies, and diverse biological activities. This study critically examines the recent advances and emerging therapeutic applications of the pyrazoline motif, with particular emphasis on structure-activity relationship (SAR) trends and synthetic methodologies, while focusing on key biological activities, including anticancer, antimicrobial, antitubercular, antioxidant, and anti-inflammatory activities. However, key challenges persist, including the development of safe, non-toxic, and environmentally sustainable synthetic procedures. A vast number of structurally complex and bulky frameworks remain largely unexplored in this regard. Additionally, there is a pressing need for efficient in vitro and in vivo screening methodologies that can effectively validate relevant biological targets. This review will be helpful for the rational design of new pyrazoline-based molecules that could be used in the future to synthesize them by performing further modifications and selecting suitable synthetic strategies to develop next-generation pyrazoline derivatives with enhanced therapeutic potential.