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

摘要

A series of 7-substituted-benzylamino-4, 5-dihydro-[l, 2, 4]triazolo[4, 3-a]quinoline derivatives was synthesized and e valuated 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-[l, 2,4]triazolo[4, 3-a]quinoline (4j) with an ED_(50) 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 ED_(50) 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 neurotoxici ty test, and the results showed that all derivatives possessed lower neurotoxicity.