Microwave-assisted synthesis and anticonvulsant activity of 5,6-bisaryl-1,2,4-triazine-3-thiol derivatives

作者：Irannejad Hamid^*; Naderi Nima; Emami Saeed; Ghadikolaei Roja Qobadi; Foroumadi Alireza; Zafari Tina; Mazar Atabaki Ali; Dadashpour Sakineh

来源：Medicinal Chemistry Research, 2014, 23(5): 2503-2514.

DOI：10.1007/s00044-013-0843-6

• Anticonvulsant activity
• Microwave synthesis
• Mixed-green solvent system
• 1,2,4-Triazine, distance mapping

A series of 5,6-bisaryl-1,2,4-triazine-3-thiol derivatives were synthesized through microwave-promoted chemistry by condensation of the aromatic 1,2-diketones and thiosemicarbazide in a mixed green solvent. Subsequently, S-alkylation of 1,2,4-triazine-3-thiols afforded S-substituted derivatives. The anticonvulsant activity of the synthesized compounds was evaluated in vivo by electroshock and pentylenetetrazole (PTZ)-induced seizures tests. Among them, compound 4a bearing 4-pyridylmethylthio moiety on the triazine ring showed the highest protection in both electroshock and PTZ-induced seizures tests. Compound 4a showed no sign of neurotoxicity at the dose of 100 mg/kg in both rotarod and chimney tests.

• 出版日期2014-5