Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.

Gianotti, Massimo; Corti, Corrado; Delle Fratte, Sonia; Di Fabio, Romano; Leslie, Colin P; Pavone, Francesca; Piccoli, Laura; Stasi, Luigi; Wigglesworth, Mark J

Gianotti, Massimo; Corti, Corrado; Delle Fratte, Sonia; Di Fabio, Romano; Leslie, Colin P; Pavone, Francesca; Piccoli, Laura; Stasi, Luigi; Wigglesworth, Mark J.

Afiliación

Gianotti M; Neurosciences CEDD, GlaxoSmithKline, Medicines Research Centre, Verona, Italy. massimo.gianotti@aptuit.com

Bioorg Med Chem Lett ; 20(17): 5069-73, 2010 Sep 01.

Article en En | MEDLINE | ID: mdl-20674357

RESUMEN

A novel imidazobenzazepine template (5a) with potent dual H(1)/5-HT(2A) antagonist activity was identified. Application of a zwitterionic approach to this poorly selective and poorly developable starting point successfully delivered a class of high quality leads, 3-[4-(3-R(1)-2-R-5H-imidazo[1,2-b][2]benzazepin-11-yl)-1-piperazinyl]-2,2-dimethylpropanoic acids (e.g., 9, 19, 20, and 21), characterized by potent and balanced H(1)/5-HT(2A) receptor antagonist activities and good developability profiles.

Asunto(s)

Receptor de Serotonina 5-HT1A/efectos de los fármacos; Receptor de Serotonina 5-HT2A/efectos de los fármacos; Antagonistas de la Serotonina/uso terapéutico; Trastornos del Sueño-Vigilia/tratamiento farmacológico; Humanos

Texto completo

Añadir a Mi BVS

Imprimir

XML

PubMed Links

Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antagonistas de la Serotonina / Trastornos del Sueño-Vigilia / Receptor de Serotonina 5-HT1A / Receptor de Serotonina 5-HT2A Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2010 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Reino Unido

Texto completo

Añadir a Mi BVS

Imprimir

XML

PubMed Links

Buscar en Google