1.
Int J Cardiol
; 182: 4-5, 2015 Mar 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-25597979
2.
Bioorg Med Chem Lett
; 13(6): 1001-4, 2003 Mar 24.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12643898
RESUMO
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 alpha-chloroacetamido 13 and the chloropyrimidine derivative 11 as potential site-directed probes for the epibatidine binding site.