772-55-4Relevant academic research and scientific papers
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
Patel, Hardik J.,Sarra, Joe,Caruso, Francesco,Rossi, Miriam,Doshi, Utkarsh,Stephani, Ralph A.
, p. 4644 - 4647 (2007/10/03)
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 ED50 of 41.8 mg/kg in scPTZ convulsion model.
1-arylpyrimidine derivatives and pharmaceutical use thereof
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, (2008/06/13)
The present invention relates to 1-arylpyrimidine derivatives represented by general formula (I): STR1 wherein R1 is H, alkyl or aralkyl; Ar is 1-naphthyl, or a substituted or unsubstituted phenyl group; R4 is a substituted phenyl, a substituted styryl, 1-methylcyclohexyl, 4-methylcyclohexyl, 4-oxo-4H-pyran-2-yl or 2-oxo-2H-pyran-5-yl group; R5 and R6 are each independently H or alkyl; R3 is H, and R7 and R8 are combined together to be oxo, or else R3 and R7 are combined together to be another direct bond, and R5 and R8 are combined together to be a direct bond, or pharmaceutically acceptable salts thereof; and methods for treating allergic diseases with such compounds.
