An investigation into the structure-activity relationships associated with the systematic modification of the ß(2)-adrenoceptor agonist indacaterol.
Bioorg Med Chem Lett
; 22(19): 6280-5, 2012 Oct 01.
Article
en En
| MEDLINE
| ID: mdl-22932315
The synthesis of a series of indacaterol analogues in which each of the three structural regions of indacaterol are modified in a systematic manner is described. Evaluation of the affinity of these analogues for the ß(2)-adrenoceptor identified the 3,4-dihydroquinolinone and 5-n-butylindanyl analogues to demonstrate the most similar profiles to indacaterol. An α-methyl aminoindane analogue was discovered to be 25-fold more potent than indacaterol, and functional studies revealed an atypical ß(2)-adrenoceptor activation profile for this compound consistent with that of a slowly dissociating 'super agonist'.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Receptores Adrenérgicos beta 2
/
Quinolonas
/
Agonistas de Receptores Adrenérgicos beta 2
/
Indanos
Tipo de estudio:
Risk_factors_studies
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2012
Tipo del documento:
Article
País de afiliación:
Reino Unido
Pais de publicación:
Reino Unido