Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione-Based Compounds

Molecules

Tomasz Plech¹  Barbara Kaproń¹  Jarogniew J. Łuszczki⁴  Monika Wujec¹  Agata Paneth¹  Agata Siwek²  Marcin Ko𔊬zkowski³  Maria Żołnierek² 

[1] Department of Organic Chemistry, Medical University of Lublin, Chodźki 4a, Lublin 20-093, Poland; E-Mails:;Department of Pharmacobiology, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland; E-Mails:;Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland; E-Mail:;Department of Pathophysiology, Medical University of Lublin, Jaczewskiego 8, Lublin 20-090; Poland; E-Mail:

关键词: 30-688 s-triazoles;    Mannich bases;    maximal electroshock-induced seizure (MES) test;    blood-brain barrier (BBB);    radioligand binding assay;   

DOI  :  10.3390/molecules190811279

来源: mdpi

【 摘 要 】

The anticonvulsant activity of several 1,2,4-triazole-3-thione derivatives on mouse maximal electroshock-induced seizures was tested in this study. Characteristic features of all active compounds were rapid onset of action and long lasting effect. Structure-activity observations showed that the probability of obtaining compounds exerting anticonvulsant activity was much higher when at least one of the phenyl rings attached to 1,2,4-triazole nucleus had a substituent at the para position. The obtained results, moreover, permit us to conclude that despite the structural similarity of loreclezole (second-generation anticonvulsant drug) and the titled compounds, their anticonvulsant activity is achieved via completely different molecular mechanisms.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.