Synthesis and anticonvulsant activity of 7-benzylamino-4,5-dihydro-［1,2,4］triazolo［4,3-a］quinolines

A series of 7-substituted-benzylamino-4,5-dihydro-［1,2,4］triazolo［4,3-a］quinoline derivatives was synthesized and evaluated for their anticonvulsant activity. The subcutaneous pentylenetetrazole test (sc-PTZ) demonstrated that the most effective compound in controlling the sc-PTZ induced seizure was 7-(3-bromine-benzylamino)-4,5-dihydro-［1,2,4］triazolo［4,3-a］quinoline (4j) with an ED₅₀ of 5.0 mg/kg and the PI of 20.7, which was also safer than the reference drugs. And the maximal electroshock test (MES) demonstrated that among these derivatives, 7-(3-fluorobenzylamino) -4,5-dihydro-［1,2,4］trizolo［4,3-a］quinoline (4i), with an ED₅₀ of 15.3 mg/kg and the PI of 7.2, was the safest in MES test. Furthermore, their neurotoxicities were measured by the rotarod neurotoxicity test, and the results showed that all derivatives possessed lower neurotoxicity.