Synthesis of Novel 8-alkylamino-5, 6-dihydro-4H-benzo[f] [1,2,4]triazolo [4,3-a]azepines as Anticonvulsant Agents

Author(s): Hui-Fan Wu, Rong-Bi Han, Chun-Zi Jin, Feng-Yu Piao.

Journal Name: CNS & Neurological Disorders - Drug Targets

Volume 15 , Issue 10 , 2016

Become EABM
Become Reviewer

Abstract:

A series of new 8-alkylamino-5, 6-dihydro-4H-benzo[f][1,2,4]triazolo [4,3-a]azepine derivatives were synthesized and screened for their anticonvulsant activities by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. The results of these tests showed that 8-heptylamino-5,6- dihydro-4H-benzo[f][1,2,4] triazolo[4,3-a]azepine (7g) was the most promising compound, with median effective dose (ED50) of 19.0 mg/kg, and protective index (PI) value of 14.8 in the MES test, which is much higher than the PI value of the prototype antiepileptic drug carbamazepine (PI = 8.1), phenytoin (PI = 6.9), phenobarbital (PI = 3.2), and sodium valproate (PI = 1.6). The possible structure–activity relationship was discussed.

Keywords: Anticonvulsant activity, Benzotriazoloazepine, Synthesis, Triazole, Toxicity.

Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 15
ISSUE: 10
Year: 2016
Page: [1333 - 1343]
Pages: 11
DOI: 10.2174/1871527315666160321111211
Price: $58

Article Metrics

PDF: 16
HTML: 4
EPUB: 1
PRC: 1