Design Synthesis and in Vitro Evaluation of Oxadiazole Analogues for the Management of Cognitive Dysfunction

Abstract

Oxadiazoles are a prominent class of heterocyclic compounds that have garnered significant attention in pharmaceutical science due to their diverse biological activities. This thesis focuses on the synthesis and characterization of 5- substituted-1,3,4-oxadiazole-2-thione, 5-substituted 1,3,4-thiadiazoles, 2-amino- 5-substituted-1,3,4- thiadiazoles, which have been explored for their potential antioxidant, antibacterial, anti-fungal, anxiolytic activities. A four-step synthetic route was employed to obtain the target compounds, which were subsequently characterized using spectral analysis. newlineThe present investigation aims to contribute to the understanding of the structure- activity relationships of these derivatives and their potential applications in drug discovery. The synthesized compounds were evaluated for their ability to bind with AChE and COX-2 enzymes was evaluated by various biochemical assays. Molecules displaying potential ability to inhibit AChE and COX-2 were evaluated further using in vivo behavioral studies. newlineThe in vitro Anti-oxidant activities of synthesized compounds was determined using DPPH methods. The % inhibition of 13f was found maximum (51.36%) followed by 11f (44.28 %) when compared with other compounds. Similarly, Anti-microbial activity of synthesized compounds indicated that % inhibition of 11f and 13f was found maximum. The in vivo behavioural study indicate that the compound 11f and 13f found to have significant (P lt 0.05) anxiolytic activity. The 13f compound showed maximum activity when compared with standard drug and 11f. newlineThis research provides insights into the design and synthesis of novel oxadiazole derivatives and their potential as lead molecules for the development of new anxiolytic agents.