Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines.
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.
Xie
Zhi-Feng
ZF
College of Pharmacy, Yanbian University, Yanji, Jilin 133000, PR China.
Chai
Kyu-Yun
KY
Piao
Hu-Ri
HR
Kwak
Kyung-Chell
KC
Quan
Zhe-Shan
ZS
D000818:Animals; D000927:Anticonvulsants / Q000009:adverse effects / Q000138:chemical synthesis* / Q000494:pharmacology; D004195:Disease Models, Animal; D051379:Mice; D020258:Neurotoxicity Syndromes; D011804:Quinolines / Q000009:adverse effects / Q000138:chemical synthesis* / Q000494:pharmacology; D012640:Seizures / Q000188:drug therapy; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D011804:Quinolines