Synthesis and Evaluation of Anticonvulsant Activity of Schiff Base of 1,4-Benzodiazepine Amine.

Synthesis and Evaluation of Anticonvulsant Activity of Schiff Base of 1,4-Benzodiazepine Amine. Chem Biodivers. 2020 Jun 29;: Authors: Gawande MB, Nilkanth PR, Ghorai S, S A, Dhawale K, Shelke S, Ahamad T Abstract A variety of 1,4-benzodiazepine azomethines (3a-n) and 1,4-benzodiazepine benzamide (4) were prepared, characterized and evaluated for the anticonvulsant activity in the rat using picrotoxin-induced seizure model. The prepared 1,4-benzodiazepine azomethine derivative emerged potentially anticonvulsant molecular scaffolds exemplified by compounds, 7-(4-nitrophenyl)methyleneamino-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one (3c), 7-[4-(dimethylamino)phenyl]methyleneamino-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one (3e), 7-[(4-bromo-2,6-difluoro-phenyl)methyleneamino]-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one (3l) and 7-[3-(4-fluorophenyl)-1-phenyl-pyrazol-4-yl]methyleneamino-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one (3n). All these four compounds have shown substantial decrease in the wet dog shake numbers and grade of convulsions with respect to the standard drug diazepam. Most active compound, 7-[4-(dimethylamino)phenyl]methyleneamino-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one (3e) exhibits 74 % protection against convulsion which was higher than standard drug diazepam. Furthermore, to identify the binding mode of the interaction amongst the target analogs and binding site of the benzodiazepine receptor, molecular ...
Source: Chemistry and Biodiversity - Category: Biochemistry Authors: Tags: Chem Biodivers Source Type: research