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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
Author(s) -
Madaiah Malavalli,
Prashanth Maralekere K.,
Revanasiddappa Hosakere D.,
Veeresh Bantal
Publication year - 2014
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201300289
Subject(s) - pentylenetetrazol , imidazolidine , phenytoin , anticonvulsant , chemistry , neurotoxicity , potency , stereochemistry , chemical synthesis , pharmacology , octane , epilepsy , toxicity , biochemistry , organic chemistry , medicine , in vitro , psychiatry
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 and spectral data. The novel molecules were screened for anticonvulsant activity in mice by maximal electroshock (MES) and subcutaneous pentylenetetrazol (ScPTZ)‐induced seizure tests. The neurotoxicity was assessed using the rotarod method. Compounds 9 , 10 , 18 , 30 , and 31 exhibited anticonvulsant potency against MES seizure and in the ScPTZ model, with lesser neurotoxicity. Some title compounds showed lesser central nervous system depression compared to phenytoin.