Type of Document Master's Thesis Author White, David Charles Author's Email Address firstname.lastname@example.org 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
- antiepileptic drugs
Date of Defense 1997-08-21 Availability restricted AbstractA 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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