Zhe-Shan Quan, Jun-min Wang, J. Rho
2005
Citations
0
Influential Citations
26
Citations
Quality indicators
Journal
Bulletin of The Korean Chemical Society
Abstract
A series of 6-alkyloxyl-3,4-dihydro-2(1H)-quinoliones (5a-5n) were synthesized through nitration, reduction, diazotization, hydrolysis and alkylation from 3,4-dihydro-2(lH)-quinolione. Their structures were characterized by IR, 1 H-NMR and MS. The anticonvulsant activity was evaluated by the Maximal electroshock test (MES) and the subcutaneous pentylenetetrazole (Metrazole) test (sc-Met). The neurotoxicity was measured by the Rotarod test (Tox). The result showed that 6-hexyloxy-3,4-dihydro-2 (1H)-quinolinone (5c) was potent in anti-MES and anti-scMet test with ED 5 0 of 24.0 mg/kg and 21.2 mg/kg, respectively, albeit its TD 5 0 (67.6 mg/kg) revealed the high neurotoxicity. 6-Benzyloxy-3,4-dihydro-2(1H)-quinolinone (5f) was less effective against MES induced seizure with ED 5 0 of 29.6 mg/kg, but no neurotoxicity was observed even under 300 mg/ kg. Its Protective index (PI) was greater than 10 preferable to Phenytoin, Carbamazepin, Phenobarbital and Valproate.