1.
Bioorg Med Chem Lett
; 17(5): 1403-7, 2007 Mar 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17178222
RESUMEN
We have modified the previously reported 2-aminoquinoline 1 to provide two novel series of MCH-1R antagonists. Representative compounds from the quinazoline and benzimidazole series have been shown to be potent and selective, with promising in vitro eADME profiles.
Asunto(s)
Bencimidazoles/síntesis química , Quinazolinas/síntesis química , Receptores de Somatostatina/antagonistas & inhibidores , Bencimidazoles/farmacología , Humanos , Concentración 50 Inhibidora , Unión Proteica , Quinazolinas/farmacología , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 14(15): 4099-102, 2004 Aug 02.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15225734
RESUMEN
A new series of 2-aminoquinolines has been identified as antagonists of the melanin concentrating hormone receptor (MCH-1R). Syntheses and structure-activity relationships are described leading to a compound having low nanomolar activity against the receptor and demonstrating functional antagonism. Studies also showed that some of the compounds were selective against a range of other G protein-coupled receptors.
