Literature

Abstract

A series of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline derivatives was synthesized using 6-hydroxy-3,4-dihydro-1H-quinolin-2-one as a starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES test) and the subcutaneous (s.c.) pentylenetetrazol test (scMet test), and their neurotoxicity was evaluated by the rotarod neurotoxicity test (Tox). MES and scMet tests show that 7-(4-fluorobenzyloxy)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline 4l was found to be the most potent with ED50 value of 11.8 and 6.7 mg kg(-1) and protective index (PI = TD50/ED50) value of 4.6 and 8.1, respectively.

DOI： 10.1016/j.bmcl.2005.07.051

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

Bioorganic & Medicinal Chemistry Letters 2005.0

Synthesis and anticonvulsant evaluation of 4-(4-alkoxylphenyl)-3-ethyl-4H-1,2,4-triazoles as open-chain analogues of 7-alkoxyl-4,5-dihydro[1,2,4]triazolo[4,3-a]quinolines

Bioorganic & Medicinal Chemistry 2007.0

Synthesis and anticonvulsant evaluation of 3-substituted-4-(4-hexyloxyphenyl)-4H-1,2,4-triazoles

Medicinal Chemistry Research 2009.0

Synthesis and anticonvulsant activity of 8-alkoxy-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a]azepine derivatives

Medicinal Chemistry Research 2012.0

Design and synthesis of some novel 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2yl]-2-phenylquinazoline-4(3H)-ones as possible anticonvulsant agent

Medicinal Chemistry Research 2011.0

Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents