Next Article in Journal
Controlled Release of Biological Control Agents for Preventing Aflatoxin Contamination from Starch–Alginate Beads
Previous Article in Journal
Black Ginseng and Its Saponins: Preparation, Phytochemistry and Pharmacological Effects
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
Molecules
Volume 24
Issue 10
10.3390/molecules24101857
molecules-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite question_answer Discuss in SciProfiles
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
Article

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

by
Shiben Wang
1,*,
Hui Liu
2,
Xuekun Wang
1,
Kang Lei
1,
Guangyong Li
1 and
Zheshan Quan
3
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
Submission received: 17 April 2019 / Revised: 9 May 2019 / Accepted: 14 May 2019 / Published: 14 May 2019
Browse Figures
Review Reports Versions Notes

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.
Keywords: synthesis; antidepressant; FST; 5-HT; molecular docking studies synthesis; antidepressant; FST; 5-HT; molecular docking studies

Share and Cite

MDPI and ACS Style

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. https://doi.org/10.3390/molecules24101857

AMA Style

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(10):1857. https://doi.org/10.3390/molecules24101857

Chicago/Turabian Style

Wang, Shiben, Hui Liu, Xuekun Wang, Kang Lei, Guangyong Li, and Zheshan Quan. 2019. "Synthesis and Evaluation of Antidepressant Activities of 5-Aryl-4,5-dihydrotetrazolo [1,5-a]thieno[2,3-e]pyridine Derivatives" Molecules 24, no. 10: 1857. https://doi.org/10.3390/molecules24101857

APA Style

Wang, S., Liu, H., Wang, X., Lei, K., Li, G., & Quan, Z. (2019). Synthesis and Evaluation of Antidepressant Activities of 5-Aryl-4,5-dihydrotetrazolo [1,5-a]thieno[2,3-e]pyridine Derivatives. Molecules, 24(10), 1857. https://doi.org/10.3390/molecules24101857

Article Metrics

Back to TopTop