Type of Document	Master's Thesis
Author	White, David Charles
Author's Email Address	white@novell.chem.utk.edu
URN	etd-72297-15249
Title	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
Degree	Master of Science
Department	Chemistry
Advisory Committee	Advisor Name Title Anderson, Mark R. Calter, Michael A. Wolfe, James F. Committee Chair
Keywords	anticonvulsants antiepileptic drugs pyridopyrimidones
Date of Defense	1997-08-21
Availability	restricted
Abstract 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.
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