A new class of histamine H3 receptor antagonists derived from ligand based design.
Bioorg Med Chem Lett
; 17(13): 3670-5, 2007 Jul 01.
Article
en En
| MEDLINE
| ID: mdl-17498953
ABSTRACT
Design and synthesis of highly potent and selective non-imidazole inverse agonists for the histamine H(3) receptor is described. The study validates a new pharmacophore model based on the merging of two previously described models. It also demonstrates that the removal of the basic center potentially interacting with ASP3.32 and common to both models leads to loss of activity, whereas the replacement of the second basic center by an acceptor retains the potency.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Química Farmacéutica
/
Receptores Histamínicos H3
/
Antagonistas de los Receptores Histamínicos
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2007
Tipo del documento:
Article
País de afiliación:
Suiza