RESUMEN
The pharmacokinetic based optimisation of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 24 was found to be a highly potent and selective cannabinoid CB(1) antagonist with high predicted human oral bioavailability.
Asunto(s)
Indoles/farmacocinética , Receptor Cannabinoide CB1/antagonistas & inhibidores , Administración Oral , Disponibilidad Biológica , Humanos , Indoles/administración & dosificación , Indoles/química , Relación Estructura-ActividadRESUMEN
The discovery and structure-activity relationship of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 26i was found to be a high potency, selective cannabinoid CB(1) antagonist.
Asunto(s)
Amidas/química , Indoles/química , Receptor Cannabinoide CB1/antagonistas & inhibidores , Amidas/síntesis química , Amidas/farmacocinética , Animales , Perros , Evaluación Preclínica de Medicamentos , Indoles/síntesis química , Indoles/farmacocinética , Masculino , Ratones , Modelos Moleculares , Ratas , Ratas Wistar , Receptor Cannabinoide CB1/metabolismo , Relación Estructura-ActividadAsunto(s)
Cannabinoides/química , Cannabinoides/farmacología , Investigación , Animales , Agonistas de Receptores de Cannabinoides , Humanos , Imidazoles/química , Imidazoles/farmacología , Inhibidores de Proteasas/química , Inhibidores de Proteasas/farmacología , Receptores de Cannabinoides/metabolismo , Relación Estructura-ActividadRESUMEN
On December 2, 2004, the Society for Medicines Research held the seventh Trends in Medicinal Chemistry one-day meeting. The meeting brought together speakers from Europe representing both academia and industry and provided an overview of some of the latest approaches being taken in a range of therapeutic areas such as oncology, antiinfectives, CNS disease and reproductive medicine.
Asunto(s)
Investigación Biomédica/tendencias , Química Farmacéutica/tendencias , Quimioterapia/tendencias , Sociedades Científicas , Animales , Congresos como Asunto , Humanos , Reino UnidoRESUMEN
A series of 3-phenoxypropyl piperidine analogues have been discovered as novel ORL1 receptor agonists. Structure-activity relationships have been explored around the 3-phenoxypropyl region with several potent and selective analogues identified.
