This proposal deals with the synthesis of new anticonvulsant drugs. The synthetic procedures to be employed involve new carbanion intermediates derived from compounds having a molecular framework common to several known classes of anticonvulsant agents as well as carbanions which can be used to construct such molecules. Special emphasis will be placed on the preparation of novel compounds, which cannot be synthesized by current techniques for construction of the parent molecule, and on introduction of specific pharmacophoric groups into the parent compounds. Included as synthetic goals are new compounds of the following structural types: (1)-[2-oxo-2-(4-pyridyl)ethyl]-3-aryl-4(3H)-quinazolinones and related compounds; (2) Alpha-substituted, Alpha, Alpha-disubstituted, and fused-ring derivatives of glutarimide and succinimide; (3) Alpha-benzyl Gamma-butyrolactones and Delta-valerolactones; (4) 1,3-dihydro-2H-1,4-benzodiazepin-2-ones and 1,5-dihydro-2H-1, 4-benzodiazepin-2-ones; (5) Alpha-substituted and Alpha, Alpha-disubstituted 6-chloro-2H-1,4-benzoxazine-3(4H)-ones and benzothiazinone dioxides; and (6) N-phenylacetyl derivatives of trifluoromethanesulfonamide and other sulfonamides related to azetazolamide and sulthimine.

Agency
National Institute of Health (NIH)
Institute
National Institute of Neurological Disorders and Stroke (NINDS)
Type
Research Project (R01)
Project #
5R01NS010197-10
Application #
3394157
Study Section
Medicinal Chemistry Study Section (MCHA)
Project Start
1978-12-01
Project End
1986-11-30
Budget Start
1985-12-01
Budget End
1986-11-30
Support Year
10
Fiscal Year
1986
Total Cost
Indirect Cost
Name
Virginia Polytechnic Institute and State University
Department
Type
Schools of Arts and Sciences
DUNS #
003137015
City
Blacksburg
State
VA
Country
United States
Zip Code
24060