Design and Synthesis of Novel Diphenyl Oxalamide and Diphenyl Acetamide Derivatives as Anticonvulsants

A series of novel N1‐substituted‐N2,N2‐diphenyl oxalamides 3a–l were synthesized in good yield by stirring diphenylcarbamoyl formyl chloride (2) and various substituted aliphatic, alicyclic, aromatic, heterocyclic amines in DMF and K2CO3. Also 2‐substituted amino‐N,N‐diphenylacetamides 5a–m were des...

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Veröffentlicht in:Archiv der Pharmazie (Weinheim) 2012-01, Vol.345 (1), p.57-64
Hauptverfasser: Nikalje, Anna Pratima G., Ghodke, Mangesh, Girbane, Amol
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Sprache:eng
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Zusammenfassung:A series of novel N1‐substituted‐N2,N2‐diphenyl oxalamides 3a–l were synthesized in good yield by stirring diphenylcarbamoyl formyl chloride (2) and various substituted aliphatic, alicyclic, aromatic, heterocyclic amines in DMF and K2CO3. Also 2‐substituted amino‐N,N‐diphenylacetamides 5a–m were designed by pharmacophore generation and synthesized by stirring 2‐chloro‐N,N‐diphenylacetamide (4) and various substituted amines in acetone using triethyl amine as a catalyst. All the synthesized compounds were screened for anticonvulsant activity in Swiss albino mice by MES and ScPTZ induced seizure tests. Neurotoxicity screening and behavioral testing was also carried out. Some of the synthesized test compounds were found to be more potent than the standard drug. A series of novel N1‐substituted‐N2,N2‐diphenyl oxalamide and 2‐substituted amino‐N,N‐diphenyl acetamide derivatives was synthesized and evaluated for their anticonvulsant, CNS depressant activity and neurotoxicity
ISSN:0365-6233
1521-4184
DOI:10.1002/ardp.201100108