Synthesis and Pharmacological Evaluation of Novel 1′-[2-(Difluoromethoxy)benzyl]-2′H,5′H-spiro[8-azabicyclo[3.2.1]octane-3,4′-imidazolidine]-2′,5′-diones and Their Derivatives

作者: Malavalli Madaiah , Maralekere K Prashanth , Hosakere D Revanasiddappa , Bantal Veeresh

DOI: 10.1002/ARDP.201300289

关键词: AnticonvulsantPhenytoinImidazolidineChemistryPotencyNeurotoxicityStereochemistryOctaneIsocyanatePentylenetetrazol

摘要: A series of novel 1'-[2-(difluoromethoxy)benzyl]-2'H,5'H-spiro[8-azabicyclo[3.2.1]octane-3,4'-imidazolidine]-2',5'-dione substituted hydantoins (5-32) were synthesized using an appropriate synthetic route and characterized by elemental analysis spectral data. The molecules screened for anticonvulsant activity in mice maximal electroshock (MES) subcutaneous pentylenetetrazol (ScPTZ)-induced seizure tests. neurotoxicity was assessed the rotarod method. Compounds 9, 10, 18, 30, 31 exhibited potency against MES ScPTZ model, with lesser neurotoxicity. Some title compounds showed central nervous system depression compared to phenytoin.

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