Synthesis and binding affinity of new 1,4-disubstituted triazoles as potential dopamine D(3) receptor ligands.
Bioorg Med Chem Lett
; 23(20): 5586-91, 2013 Oct 15.
Article
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| MEDLINE
| ID: mdl-24012118
ABSTRACT
A series of new 1,4-disubstituted triazoles was prepared from appropriate arylacetylenes and aminoalkylazides using click chemistry methodology. These compounds were evaluated as potential ligands on several subtypes of dopamine receptors in in vitro competition assays, showing high affinity for dopamine D3 receptors, lower affinity for D2 and D4, and no affinity for the D1 receptors. Compound 18 displayed the highest affinity at the D3 receptor with a Ki value of 2.7 nM, selectivity over D2 (70-fold) and D4 (200-fold), and behaviour as a competitive antagonist in the low nanomolar range.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Piperazinas
/
Triazoles
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Receptores de Dopamina D3
/
Ligandos
Límite:
Humans
Idioma:
En
Año:
2013
Tipo del documento:
Article