Novel conformationally constrained analogues of agomelatine as new melatoninergic ligands.
Molecules
; 18(1): 154-66, 2012 Dec 24.
Article
en En
| MEDLINE
| ID: mdl-23262445
ABSTRACT
Novel conformationally restricted analogues of agomelatine were synthesized and pharmacologically evaluated at MT1 and MT2 melatoninergic receptors. Replacement of the N-acetyl side chain of agomelatine by oxathiadiazole-2-oxide (compound 3), oxadiazole-5(4H)-one (compound 4), tetrazole (compound 5), oxazolidinone (compound 7a), pyrrolidinone (compound 7b), imidazolidinedione (compound 12), thiazole (compounds 13 and 14) and isoxazole moieties (compound 15) led to a decrease of the melatoninergic binding affinities, particularly at MT1. Compounds 7a and 7b exhibiting nanomolar affinity towards the MT2 receptors subtypes have shown the most interesting pharmacological results of this series with the appearance of a weak MT2-selectivity.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Receptor de Melatonina MT1
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Receptor de Melatonina MT2
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Acetamidas
Límite:
Animals
Idioma:
En
Revista:
Molecules
Asunto de la revista:
BIOLOGIA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Francia