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Synthesis and Biological Evaluation of Some Schiff’s Bases of 2-Substituted-1, 3, 4-Oxadiazole


Affiliations
1 Department of Medicinal Chemistry, Bharati Vidyapeeth’s College of Pharmacy, C.B.D., Belapur, Navi Mumbai-400614, India
     

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The present research work is oriented towards the synthesis of coupled heterocyclic system and its subsequent conversion into Schiff's bases. Ethyl-5-N′-(1,2,4-triazolyl)-acetate 1 was converted in to its hydrazide by heating with hydrazine hydrate. Hydrazide was further cyclised to 2-amino-5-(N′-1,2,4-triazolomethyl)-1,3,4-oxadiazole 3, which upon further treatment with various aromatic aldehydes under acidic condition afforded corresponding Schiff's bases 4a-4j. All compounds were screened for anticonvulsant activity by MES method.

Graphical abstract:

Hitherto unreported Schiff's bases 4a-4j of 1,2,4-triazolo substituted 1,3,4-oxadiazole amine 3 are prepared under acidic conditions. The newly synthesized compounds are characterized by spectral analyses. All the compounds are screened for anticonvulsant activity using MES method. 4d exhibited promising anticonvulsant activity, whereas others have shown moderate activity.


Keywords

Synthesis, 1,3,4-Oxadiazole, 1,2,4-Triazole, Schiff’s Bases, Anti-Convulsant.
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  • Synthesis and Biological Evaluation of Some Schiff’s Bases of 2-Substituted-1, 3, 4-Oxadiazole

Abstract Views: 256  |  PDF Views: 1

Authors

Kishore U. Kothule
Department of Medicinal Chemistry, Bharati Vidyapeeth’s College of Pharmacy, C.B.D., Belapur, Navi Mumbai-400614, India
Prashant Kesharwani
Department of Medicinal Chemistry, Bharati Vidyapeeth’s College of Pharmacy, C.B.D., Belapur, Navi Mumbai-400614, India
Rakesh R. Somani
Department of Medicinal Chemistry, Bharati Vidyapeeth’s College of Pharmacy, C.B.D., Belapur, Navi Mumbai-400614, India
Prabhakar Y. Shirodkar
Department of Medicinal Chemistry, Bharati Vidyapeeth’s College of Pharmacy, C.B.D., Belapur, Navi Mumbai-400614, India

Abstract


The present research work is oriented towards the synthesis of coupled heterocyclic system and its subsequent conversion into Schiff's bases. Ethyl-5-N′-(1,2,4-triazolyl)-acetate 1 was converted in to its hydrazide by heating with hydrazine hydrate. Hydrazide was further cyclised to 2-amino-5-(N′-1,2,4-triazolomethyl)-1,3,4-oxadiazole 3, which upon further treatment with various aromatic aldehydes under acidic condition afforded corresponding Schiff's bases 4a-4j. All compounds were screened for anticonvulsant activity by MES method.

Graphical abstract:

Hitherto unreported Schiff's bases 4a-4j of 1,2,4-triazolo substituted 1,3,4-oxadiazole amine 3 are prepared under acidic conditions. The newly synthesized compounds are characterized by spectral analyses. All the compounds are screened for anticonvulsant activity using MES method. 4d exhibited promising anticonvulsant activity, whereas others have shown moderate activity.


Keywords


Synthesis, 1,3,4-Oxadiazole, 1,2,4-Triazole, Schiff’s Bases, Anti-Convulsant.