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Synthesis of 2‐Substituted‐7‐heptyloxy‐4,5‐dihydro‐[1,2,4]‐triazolo[4,3‐ a ]quinolin‐1(2 H )‐ones with Anticonvulsant Activity
Author(s) -
Wei ChengXi,
Li FuNan,
Zhao LongXuan,
Zhao LiMing,
Quan ZheShan
Publication year - 2007
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200700106
Subject(s) - anticonvulsant , chemistry , phenytoin , potency , carbamazepine , pharmacology , neurotoxicity , toxicity , stereochemistry , epilepsy , in vitro , medicine , biochemistry , organic chemistry , psychiatry
A series of 2‐substituted‐7‐heptyloxy‐4,5‐dihydro‐[1,2,4]triazolo[4,3‐ a ]quinolin‐1(2 H )‐ones was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test, subcutaneous pentylenetetrazole (sc‐PTZ), and rotarod tests with intraperitoneally injected mice. Among the synthesized compounds, 2‐propionyl‐7‐heptyloxy‐4,5‐dihydro‐[1,2,4]triazolo[4,3‐ a ]quinoline‐1(2 H )‐one 4b was the most active one and also had the lowest toxicity. In the anti‐MES potency test, it showed median effective dose (ED 50 ) of 8.2 mg/kg, median toxicity dose (TD 50 ) of 318.3 mg/kg, and the protective index (PI) of 39.0 which is much greater than the PI of the reference drugs phenytoin and carbamazepine.