Design, Synthesis, Characterisation & Anticonvulsant Activities of Novel Heterocyclic Substituted Isatin Derivatives
Twelve new isoxazole/pyrazole/pyrimidine substituted 5-nitrosation analogues were designed according to the requirements of the anticonvulsant drugs pharmacophore model and synthesised from indole-2,3-dione. Entire prepared compounds chemical structures were established from its IR, proton-NMR, Mass spectrum & microanalysis data. Anticonvulsant potency of final isatin analogues was assessed by MES technique & sc PTZ technique. Besides rotarod test was used to assess the neurotoxicity of all potent title analogues. Title compounds exhibited a varying degree of anticonvulsant potency ranging from mild to good. In the present study, it was concluded that pyrazole derivatives exhibited higher anti-epileptic activity than isoxazole derivatives. However, pyrimidine analogues displayed inferior activity than isoxazole analogues. 4-(2-(4-(1-((Dimethylamino)methyl)-5-nitro-2-oxindole-3-ylideneamino)phenyl) hydrazone)-1-(4-chlorophenyl)-3-amino-1H-pyrazole-5(4H)-one 7c was established as the most active analog of this series. Hence this derivative can act as a pilot molecule for further progress of new effective anticonvulsant drugs.
Keywords:Isatin, Indole-2, 3-dione, Mannich Base, Schiff Base, Isoxazole, Pyrazole, Pyrimidine, Anticonvulsant, Neurotoxicity
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