University of York Department of Chemistry

The Development of New GABA-Based Anticonvulsant Agents


Justin S. Bryans,a Nicola Chessumb and Andrew F. Parsonsb

aPfizer Global Research and Development, Sandwich, Kent, CT13 9NJ 
bDepartment of Chemistry, University of York, Heslington, York, UK YO10 5DD

 Nicola Chessum


g-Aminobutyric acid [GABA (1)] is the principal inhibitory transmitter in the mammalian central nervous system. GABA has been comprehensively studied in terms of both its biochemistry and pharmacology.
GABA

A number of drugs designed as GABA analogues have found application in the treatment of epilepsy, movement disorders and pain. Some examples are shown below.
 
 

GABA analogues

Therefore, the synthesis and screening of new compounds based on the structure of GABA is of great interest due to possible pharmacological effects. The aim of this project is to use free-radical chemistry to develop efficient routes to new cyclic and acyclic analogues of GABA.

The key step in the synthesis of these compounds centres on a radical cyclisation reaction to make substituted N-heterocycles. This cyclisation can be mediated using a variety of reagents including tributyltin hydride or copper(I) chloride/bipyridine.1 Ring-opening of the resultant N-heterocycles is expected to provide a short and flexible approach to GABA analogues.

1 Bryans J S, Chessum N E A, Parsons A F, Ghelfi F,  Tetrahedron Lett., 2001, 42, 2901-2905
 
 

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