1061-1068 Quan LAJP 3627:Quan

Latin American Journal of Pharmacy
(formerly Acta Farmacéutica Bonaerense)
Lat. Am. J. Pharm. 33 (7): 1061-8 (2014)
Regular article
Received: February 19, 2014
Revised version: May 28, 2014
Accepted: May 29, 2014
Synthesis and Evaluation of Antidepressant Activities
of 5-Alkoxy-6,7,8,9-tetrahydro-benzothieno[3,2-e]tetrazolo
[1,5-a]pyrimidine Derivatives
Shi-Ben WANG 1, Da-Chuan LIU 1, Xian-Qing DENG 2, Guo-Hua GONG 3* & Zhe-Shan QUAN 1*
1
College of Pharmacy, Yanbian University, No. 977, Park road, Yanji, Jilin, 133002, China.
2 Medical College, Jinggangshan University, Ji’an, JiangXi, 343009, China.
3 Medicinal Chemistry and Pharmacology Institute, Inner Mongolia University for the Nationalities,
No. 22 Huolin He Street, Tongliao City, Inner Mongolia, 028000, P.R. China.
SUMMARY. Twenty new 5-alkoxy-6,7,8,9-tetrahydro-benzothieno[3,2-e]tetrazolo[1,5-a]pyrimidine derivatives
were synthesised and their antidepressant activities were evaluated by forced-swimming test (FST) on kun-ming
mice. The chemical structures of the compounds were proved by means of their IR, MS, 1H-NMR and 13C-NMR
spectroscopic data. The most active compound was 5-(4-methyl-phenoxy)-6,7,8,9-tetrahydro-benzothieno[3,2-e]
tetrazolo[1,5-a]pyrimidine (6m), which decreased the immobility time by 50.81% at a dose of 50 mg/kg. The results of open-field tests of this compound indicated that it had no significant effects on the locomotor activity
compared with the control group at the doses assayed in the forced swimming test.
RESUMEN. Veinte nuevos derivados de 5-alcoxi-6,7,8,9-tetrahidro-benzotieno [3,2-e]tetrazolo[1,5-a] pirimidina
se sintetizaron y se evaluaron sus actividades antidepresivas mediante la prueba de natación forzada (FST) en ratones kun-ming. Las estructuras químicas de los compuestos se probaron por medio de su IR, MS, los datos espectroscópicos de 1H-RMN y 13C-RMN. El compuesto más activo fue de 5-(4-metil-fenoxi)6,7,8,9-tetrahidrobenzotieno[3,2-e] tetrazolo[1,5-a] pirimidina (6m), el cual redujo el tiempo de inmovilidad por 50,81% a una dosis de 50 mg/kg. Los resultados de las pruebas a campo abierto de este compuesto indicaron que no tenía ningún
efecto significativo sobre la actividad locomotora en comparación con el grupo control en las dosis ensayadas en
la prueba de natación forzada.
KEY WORDS: Antidepressant, Forced swimming test, Open-field test, Pyrimidine, Tetrazole, Thiophene.
*
Author to whom correspondence should be addressed. E-mail: [email protected], [email protected]
ISSN 0326 2383 (printed ed.)
ISSN 2362-3853 (on line ed.)
1061

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