Heterocyclic compounds constitute the largest family in organic chemistry. Their potential to treat and deter various types of diseases renders them essential compounds. Moreover, their extensive implementations in drug discovery and development are significantly contributing to the current state of medicinal chemistry. Pyridine is one of the most fundamental heterocyclic compounds. Pyridine-based compounds are structurally diverse and have been utilized to tackle various challenges in pharmaceuticals and medicinal chemistry, providing novel approaches for enhanced health accomplishments. The main objective of this review is to comprehensively clarify the crucial role of pyridine derivatives in drug discovery between 2015 and 2025 by summarizing the various synthetic pathways and evaluating their therapeutic relevance. In addition, it highlights the outstanding pharmacological applications of pyridine-containing compounds across a broad range of therapeutic areas, such as oncology, infectious diseases, inflammatory disorders, oxidative stress-related conditions, metabolic disorders, and neurodegenerative diseases, emphasizing their prominence among clinically approved drugs. Furthermore, structure-activity relationship analyses are investigated to illustrate how particular substitutions, electronic effects, and positional modifications on the pyridine ring affect biological potency, selectivity, and pharmacokinetic behavior. Finally, by integrating synthetic approaches, biological evaluations, and structure-activity relationship insights, this review aims to support the rational design and optimization of more potent, selective, and safer pyridine- based therapeutic agents for future drug development.
Abdin et al. (2026) studied this question.