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filingDate 1993-09-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a411fd1777107d1ce1ba340e62a0a950
publicationDate 1994-03-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-9406758-A1
titleOfInvention Aryl semicarbazone anticonvulsants
abstract A number of aryl semicarbazones were prepared as candidate anticonvulsants. When administered orally to rats, significant activity was noted in the maximal electroshock (MES) screen and since neurotoxicity was either absent or reduced (as compared to intraperitoneal injection in mice), high protection indices were found in the majority of the compounds. The semicarbazones displayed little or no activity in the subcutaneous pentylenetetrazol screen. These observations support the theory that one large hydrophobic group (in this case the aryl ring) are requirements for protection in the MES screen. In general, the semicarbazones had rapid onsets of action and the most common mechanism of action was interaction with chloride channels. Empirical and semi-empirical conformational calculations indicated that certain molecular fragments and hydrophobicity of these molecules affect bioactivity.
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