| Document Type: | Master's Thesis |
| Name: | David Charles White |
| Email address: | white@novell.chem.utk.edu |
| URN: | 1997/00111 |
| 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 |
| Committee Chair: | Dr. James F. Wolfe |
| Chair's email: | jwolfe@vt.edu |
| Committee Members: | |
| Keywords: | anticonvulsants, antiepileptic drugs, pyridopyrimidones |
| Date of defense: | August 21, 1997 |
| Availability: | Release the entire work for Virginia Tech access only.
After one year release worldwide only with written permission of the student and the advisory committee chair. |
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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| dcw2.pdf | ||
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