Author/Authors :
Christian Che، نويسنده , , Grégory Petit، نويسنده , , Florence Kotzyba-Hibert، نويسنده , , Sonia Bertrand، نويسنده , , Daniel Bertrand، نويسنده , , Thomas Grutter، نويسنده , , Maurice Goeldner، نويسنده ,
Abstract :
The synthesis of epibatidine derivatives modified at the 2-position of the pyridine or pyrimidine rings by reactive functions are described for potential irreversible site-directed coupling reactions on cysteine mutants of neuronal nicotinic acetylcholine receptors. An improved synthesis of the 7-azabicyclo[2,2,1]hepta-2,5-diene key intermediate has been developed to allow reproducible syntheses of the epibatidine derivatives. Binding tests and electrophysiological experiments allowed to select the 2-substituted α-chloroacetamido 13 and the chloropyrimidine derivative 11 as potential site-directed probes for the epibatidine binding site.
