.7 - Alkoxy -4,5 - Dihydro-2h-[1,2,4] - Triazolo [4,3-a] Quinoline -1 - One Synthesis And Anticonvulsant Activity,

To find novel compound which have better convulsant effect and low toxicity , a series of 7-Alkyloxyl-4,5-dyhydro-[l,2,4]-thiazolo[4,3-a]quinoline-l-one derivatives was sythesized that starting with 6-hydroxyl-3,4-dihydro-2(1H)-quinoline, afford a series of unreported compound 3a-31 via alkylation, sulfide substitution and recycle. And the compound were characteried using ¹HNMR, ¹³CNMR, MS and IR, the convulsant effect and neurotoxicity were calculated with Maximal Electroshock test (MES), pentylenetetrazol and ratarod test via intraperitoneally and orally in mice.The pharmacology test displayed that the anticonvulant potency of compound 3c, 3d and 3f were comparable to the compared drugs, and ED₅₀ were 11.8mg/kg, 9.8mg/kg and 12.3mg/kg. But these compounds have remarkable low neurotoxicity compared with other marked drugs such as Phenytoin, Carbamazepine, Phenobarbital and Vaiproate, these Protect Index (PI) were 44.7, 20.8 and 44.5, but the latter were only 6.9, 8.1, 3.2 and 1.6, so these new compound 's security is better than compared durgs.Make the longest pharmacology test for compound 3f , which have the best activity , determine the median hypnosis does HD₅₀ and administered orally (po) ED₅₀, TD₅₀. Than HD₅₀ of compound 3f were 1204.6mg/kg, a greater margin of saftey (ED₅₀/TD₅₀) were 97.9, but the compared drugs of Phenytoin, Carbamazepine, Phenobarbital and Vaiproate were only 18.7, 19.5, 6.1, 3.2. These compound 's ED₅₀ and TD₅₀ is better than compared drugs by administered orally (po), these Protective Index (PI) was in excess of 44, so the compound 3f have ,a well development value.A series of thiazolo quinoline derivatives were desinged and synthesisd and found processing novel xonvulsant activity and lower neurotoxicity than markered drugs.