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Synthesis of 3-Aryl-2-(2-aryl-2-oxoethyl)pyrido[2,3-d]-4(3H)pyrimidones and 3-Aryl-2-(2-arylethenyl)pyrido[2,3-d]-4(3H)pyrimidones as Potential Antiepileptic Drugs

A series of 2-alkyl-3-arylpyrido[2,3-d]pyrimidones were synthesized for testing as potential antiepileptic drugs. The goal was to achieve better neurological activity and/or lower toxicity than displayed by a series of 2-alkyl-3-aryl-4(3H)-quinazolinones prepared previously in our research group. From the pharmacological testing data of these target compounds, we have found that the additional nitrogen at the C-8 position of the quinazolinone framework increased the anticonvulsant activity. However, the neurological toxicity increased as well. The anticonvulsant and neurotoxic activity seen in the variuos 2-alkyl side chains and 3-aryl substituents incorporated into these new pyridopyrimidones was consistent with the activity observed with the same substituents on the 4(3H)-quinazolinones. The 3-aryl group consists of various ortho-substituted phenyl rings, while the 2-alkyl chain consists of a 2-(2-aryl-2-oxo)ethyl or 2-arylethenyl group. / Master of Science

Identiferoai:union.ndltd.org:VTETD/oai:vtechworks.lib.vt.edu:10919/46506
Date26 August 1997
CreatorsWhite, David Charles
ContributorsChemistry, Wolfe, James F., Calter, Michael A., Anderson, Mark R.
PublisherVirginia Tech
Source SetsVirginia Tech Theses and Dissertation
Detected LanguageEnglish
TypeThesis
Formatapplication/pdf
RightsIn Copyright, http://rightsstatements.org/vocab/InC/1.0/
Relationdcw2.pdf

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