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Synthesis and Evaluation of Antidepressant Activities of 5-Aryl-4,5-dihydrotetrazolo [1,5-a]thieno[2,3-e]pyridine Derivatives

1
College of Pharmacy, Liaocheng University, Liaocheng 252059, China
2
College of Life Sciences, Liaocheng University, Liaocheng 252059, China
3
College of Pharmacy, Yanbian University, Yanji 133002, China
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(10), 1857; https://doi.org/10.3390/molecules24101857
Received: 17 April 2019 / Revised: 9 May 2019 / Accepted: 14 May 2019 / Published: 14 May 2019
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Abstract

In this study, we synthetized a series of 5-aryl-4,5-dihydrotetrazolo[1,5-a]thieno[2,3-e]pyridine derivatives containing tetrazole and other heterocycle substituents, i.e., triazole, methyltriazole, and triazolone. The forced swim test (FST) and tail suspension test (TST) were used to evaluate the antidepressant activity of the target compounds. The compound 5-[4-(trifluoromethyl)phenyl]-4,5-dihydrotetrazolo[1,5-a]thieno[2,3-e]pyridine (4i) showed the highest antidepressant activity, with a reduced immobility time of 55.33% when compared with the control group. Using an open-field test, compound 4i was shown to not affect spontaneous activity of mice. The determination of in vivo 5-hydroxytryptamine (5-HT) concentration showed that compound 4i may have an effect in the mouse brain. The biological activities of all synthetized compounds were verified by molecular docking studies. Compound 4i showed significant interactions with residues of the 5-HT1A receptor homology model. View Full-Text
Keywords: synthesis; antidepressant; FST; 5-HT; molecular docking studies synthesis; antidepressant; FST; 5-HT; molecular docking studies
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Wang, S.; Liu, H.; Wang, X.; Lei, K.; Li, G.; Quan, Z. Synthesis and Evaluation of Antidepressant Activities of 5-Aryl-4,5-dihydrotetrazolo [1,5-a]thieno[2,3-e]pyridine Derivatives. Molecules 2019, 24, 1857.

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