Recent Advances in Benzoxazole Synthesis: A Therapeutic Perspective on Antidepressant and Anxiolytic Activity

Abstract

Benzoxazole derivatives have garnered significant attention in medicinal chemistry due to their diverse pharmacological activities, including antimicrobial, anticancer, and notably, central nervous system (CNS) effects such as antidepressant and anxiolytic properties. Recent advancements in the synthesis of benzoxazole compounds have led to the development of novel derivatives with enhanced therapeutic potential. Studies have demonstrated that structural modifications of the benzoxazole nucleus can yield compounds exhibiting significant antidepressant-like effects in animal models. For instance, certain benzoxazole derivatives have shown high affinities for serotonin receptors, which are implicated in mood regulation, thereby producing marked antidepressant-like effects in behavioral tests such as the forced swimming test (FST) and the tail suspension test (TST). Furthermore, the incorporation of specific functional groups, such as triazole moieties, into the benzoxazole scaffold has resulted in compounds with dose-dependent antidepressant-like activity, highlighting the importance of molecular hybridization strategies in drug design. Additionally, benzoxazole derivatives have been explored for their anxiolytic potential, with certain compounds exhibiting promising activity in preclinical studies. These findings underscore the therapeutic relevance of benzoxazole-based compounds and provide a foundation for the development of new antidepressant and anxiolytic agents.​