QSAR study and molecular design of open-chain enaminones as anticonvulsant agents

Present work employs the QSAR formalism to predict the ED<SUB>50</SUB> anticonvulsant activity of ringed-enaminones, in order to apply these relationships for the prediction of unknown open-chain compounds containing the same types of functional groups in their molecular structure. Two d...

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Autores principales: Garro Martinez, Juan C., Duchowicz, Pablo Román, Estrada, Mario R., Zamarbide, Graciela N., Castro, Eduardo Alberto
Formato: Articulo
Lenguaje:Inglés
Publicado: 2011
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Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/84680
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Sumario:Present work employs the QSAR formalism to predict the ED<SUB>50</SUB> anticonvulsant activity of ringed-enaminones, in order to apply these relationships for the prediction of unknown open-chain compounds containing the same types of functional groups in their molecular structure. Two different modeling approaches are applied with the purpose of comparing the consistency of our results: (a) the search of molecular descriptors via multivariable linear regressions; and (b) the calculation of flexible descriptors with the CORAL (CORrelation And Logic) program. Among the results found, we propose some potent candidate open-chain enaminones having ED<SUB>50</SUB> values lower than 10 mg·kg<SUP>-1</SUP> for corresponding pharmacological studies. These compounds are classified as Class 1 and Class 2 according to the Anticonvulsant Selection Project.