Isoindolone derivatives, a new class of 5-HT2C antagonists: synthesis and biological evaluation.
Bioorg Med Chem Lett
; 17(2): 428-33, 2007 Jan 15.
Article
en En
| MEDLINE
| ID: mdl-17074479
Two independent approaches resulted in the identification of a series of isoindolone derivatives as potent and selective 5-HT2C antagonists. From a Medicinal Chemistry perspective this template was considered interesting as it allowed the incorporation of the carbon-carbon double bond of an earlier dihydropyrrolone series in an aromatic system within a comparatively simple and compact motif. Additionally an in silico screening approach of the corporate database using a 5-HT2C pharmacophore model resulted in the identification of a related structure containing this template. The strategy used to optimise potency at the target receptor and to improve the pharmacokinetic profile is described, resulting in molecules combining high potency with good selectivity and oral bioavailability.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Antagonistas de la Serotonina
/
Receptor de Serotonina 5-HT2C
/
Compuestos Heterocíclicos
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Indoles
Límite:
Animals
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Humans
/
Male
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2007
Tipo del documento:
Article
País de afiliación:
Italia
Pais de publicación:
Reino Unido