title: Design and synthesis of novel diphenyl oxalamide and diphenyl acetamide derivatives as anticonvulsants.
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.
authors.affiliation: Department of Pharmaceutical Chemistry, Y.B. Chavan College of Pharmacy, Aurangabad (M.S.), India. ana@k.st
authors.forename: Anna Pratima G
authors.initials: AP
authors.lastname: Nikalje
authors.forename: Mangesh
authors.initials: M
authors.lastname: Ghodke
authors.forename: Amol
authors.initials: A
authors.lastname: Girbane
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D001522:Behavior, Animal / Q000187:drug effects; D004158:Diphenylacetic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005260:Female; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D020258:Neurotoxicity Syndromes / Q000209:etiology / Q000503:physiopathology; D010072:Oxamic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D012640:Seizures / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000081:Acetamides; D000927:Anticonvulsants; D004158:Diphenylacetic Acids; D010072:Oxamic Acid; C008728:oxamide