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1.
Arch Pharm (Weinheim) ; 345(1): 57-64, 2012 Jan.
Article in English | MEDLINE | ID: mdl-21953567

ABSTRACT

A series of novel N(1) -substituted-N(2) ,N(2) -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 K(2) CO(3) . 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.


Subject(s)
Acetamides/chemical synthesis , Anticonvulsants/chemical synthesis , Diphenylacetic Acids/chemical synthesis , Drug Design , Oxamic Acid/analogs & derivatives , Acetamides/chemistry , Acetamides/therapeutic use , Acetamides/toxicity , Animals , Anticonvulsants/chemistry , Anticonvulsants/therapeutic use , Anticonvulsants/toxicity , Behavior, Animal/drug effects , Diphenylacetic Acids/chemistry , Diphenylacetic Acids/therapeutic use , Diphenylacetic Acids/toxicity , Dose-Response Relationship, Drug , Female , Male , Mice , Molecular Structure , Motor Activity/drug effects , Neurotoxicity Syndromes/etiology , Neurotoxicity Syndromes/physiopathology , Oxamic Acid/chemical synthesis , Oxamic Acid/chemistry , Oxamic Acid/therapeutic use , Oxamic Acid/toxicity , Seizures/drug therapy , Structure-Activity Relationship
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