Biol. Pharm. Bull. 28(7) 1216—1220 (2005)

characterized by epileptic seizures, which are evoked by unexpected, high-level neuronal discharges in the brain. Since the anticonvulsant agents currently used in the treatment of epilepsy have certain disadvantages such as notable side effects and inefficient therapy in some seizure types, a clear need for safer and more effective antiepileptic drugs is well known. Therefore the development of new antiepileptic drugs with approved therapeutic properties is an important challenge for medicinal chemists. The derivatives of triazole exhibit a variety of activities such as antitumor, antiinflammatory, antimicrobial, antifugal, antithrombotic, antiplatelet, antiviral, and anticonvulsant activities. In our search for new compounds with anticonvulsant activity, 6-benzyloxy-3,4-dihydro-1Hquinoline-2-one was found although its activity is low. To increase its anticonvulsant activity and taking into account the anticonvulsant activity of triazole, we incorporated triazole with 6-benzyloxy-3,4-dihydro-1H-quinolinone at the first and second position of the latter and obtained 7-benzyloxy4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline with more potent activity. To search for better compounds and elucidate structure–activity relationships, a series of 1-substituted-7-benzyloxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines was synthesized and their structures were characterized using IR, HNMR, MS, and elemental analysis techniques. The anticonvulsant activity was evaluated using the maximal eletroshock (MES) test and the subcutaneous pentylenetetrezole (sc-Met) test. Neurotoxicity was evaluated using the rotarod test. CHEMISTRY