Literature DB >> 16793262

Synthesis and anticonvulsant activity of new N-1',N-3'-disubstituted-2'H,3H,5'H-spiro-(2-benzofuran-1,4'-imidazolidine)-2',3,5'-triones.

Hardik J Patel1, Joe Sarra, Francesco Caruso, Miriam Rossi, Utkarsh Doshi, Ralph A Stephani.   

Abstract

Thirteen new N-1',N-3'-disubstituted-2'H,3H,5'H-spiro-(2-benzofuran-1,4'-imidazolidine)-2',3,5'-triones were synthesized and their pharmacological activity determined with the objective to better understand their SAR for anticonvulsant activity. The anticonvulsant effects of these compounds were evaluated by standard pentylenetetrazol (scPTZ test) and maximum electroshock seizure (MES test) models in mice. Most of the compounds showed ability to protect against the pentylenetetrazol-induced convulsions. Compound 3o (the N-1'-p-nitrophenyl, N-3'-ethyl derivative) in the N-1'-aryl, N-3'-alkyl disubstituted series exhibited maximum activity with ED(50) of 41.8 mg/kg in scPTZ convulsion model.

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Year:  2006        PMID: 16793262     DOI: 10.1016/j.bmcl.2006.05.102

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Mannich bases in medicinal chemistry and drug design.

Authors:  Gheorghe Roman
Journal:  Eur J Med Chem       Date:  2014-10-30       Impact factor: 6.514

2.  Crystal structure of 1-(5-bromo-1-benzo-furan-2-yl)ethanone oxime.

Authors:  G Krishnaswamy; P Krishna Murthy; R Nivedita Desai; P A Suchetan; D B Aruna Kumar
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-09-26
  2 in total

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