1.
Bioorg Med Chem Lett
; 18(16): 4569-72, 2008 Aug 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18662879
RESUMEN
A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential vanilloid-1 (TRPV1), an emerging target for the treatment of pain. A focused library of polar head groups led to the identification of a benzoxazinone amide that afforded good potency in cell-based assays. Synthesis and a QSAR model will be presented.
Asunto(s)
Amidas/química , Benzoxazinas/farmacología , Piperidinas/química , Canales Catiónicos TRPV/antagonistas & inhibidores , Benzoxazinas/química , Capsaicina/química , Proteínas Portadoras/antagonistas & inhibidores , Química Farmacéutica/métodos , Diseño de Fármacos , Humanos , Concentración 50 Inhibidora , Modelos Químicos , Conformación Molecular , Unión Proteica , Relación Estructura-Actividad Cuantitativa , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 18(8): 2730-4, 2008 Apr 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18359227
RESUMEN
High throughput screening of our compound library revealed a series of N-pyridyl-3-benzamides as low micromolar agonists of the human TRPV1 receptor. Synthesis of analogs in this series led to the discovery of a series of N-quinolin-3-yl-benzamides as low nanomolar antagonists of human TRPV1.
