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E u r o p e a n C o n g r e s s o n
Advanced Chemistry
Advanced Chemistry 2018
J u l y 1 2 - 1 3 , 2 0 1 8
P a r i s , F r a n c e
Page 35
Journal of Organic & Inorganic Chemistry
ISSN: 2472-1123
A
series
of
novel
5-methoxy-5,6-dihydro-4H-benzo[f][1,2,4]
triazolo[4,3-a]azepine derivatives were synthesized from
3,4-dihydronaphthalen-1(2H)-one. The structures of these compounds
were confirmed by IR,
1
H NMR,
13
C NMR, MASS spectra and elemental
analysis. Their anticonvulsant activity was evaluated 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 compound 4-hydroxyl-1, 3, 4,
5-tetrahydro-2H-1-benzazepin-2-one had moderate anticonvulsant
activities, with median effective dose (ED
50
) of 44.0 mg/kg, and
protective index (PI) value of 6.4 in the MES test. However, this
compound did not show anticonvulsant activity at the 100 mg/kg dose
level in the scPTZ test. The level of competition between the elimination
reaction and nucleophilic substitution reaction was discussed.
Synthesis and anticonvulsant activity of 5-methoxy-5,
6-dihydro-4H-benzo[f] [1, 2, 4]triazolo[4,3-a]azepine derivatives
Rui-xue Chen
1
, Rong-bi Han
1, 2
and Feng-yu Piao
1, 2
1
Yanbian University Yanji, Republic of China
2
Key Laboratory of Natural Resources of Changbai Mountain and Functional Molecules-YBU,
Republic of China
Biography
Feng-yu Piao, Yanbian University Professor, She has published more than
12 papers in reputed journals.
fypiao4989@126.comFeng-yu Piao et al., J Org Inorg Chem 2018, Volume: 4
DOI: 10.21767/2472-1123-C2-006