Synthesis of 1,3,4-oxadiazoles derivatives with antidepressant activity and their binding to the 5-HT_1A receptor.

ABSTRACT: In this study, two series of 1,3,4-oxadiazole derivatives were designed and synthesized using the forced swimming test (FST) model to test the antidepressant activity of the target compound in vivo. Five compounds with potential activity were selected from the FST model to test affinity with 5-HT_1A receptor in vitro. The results of the FST experiment showed that compound N-(3-((5-((4-chlorobenzyl)thio)-1,3,4-oxadiazol-2-yl)methoxy)phenyl)acetamide (10g) showed the best antidepressant activity (DID = 58.93, percentage decrease in immobility duration in FST), similar to the activity of positive drug fluoxetine. Compound 10g also exhibited the most potent binding affinity to 5-HT_1A receptors (K _i = 1.52 nM). The results of the in

SUBMITTER: Wang S 

PROVIDER: S-EPMC9056355 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature