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1.
Bioorg Med Chem Lett ; 29(9): 1143-1147, 2019 05 01.
Artículo en Inglés | MEDLINE | ID: mdl-30833109

RESUMEN

Selective N-methyl-d-aspartate receptor subunit 2B (NR2B) antagonists show potential as analgesic drugs, and do not cause side effects associated with non-selective N-methyl-d-aspartate (NMDA) antagonists. Using a scaffold-hopping approach, we previously identified isoxazole derivative 4 as a potent selective NR2B antagonist. In this study, further scaffold hopping of isoxazole derivative 4 and optimization of its pharmacokinetic profile led to the discovery of the orally bioavailable compound 6v. In a rat study of analgesia, 6v demonstrated analgesic effects against neuropathic pain.


Asunto(s)
Analgésicos/síntesis química , Analgésicos/farmacología , Diseño de Fármacos , Receptores de N-Metil-D-Aspartato/antagonistas & inhibidores , Analgésicos/química , Analgésicos/farmacocinética , Animales , Masculino , Estructura Molecular , Ratas , Ratas Sprague-Dawley , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett ; 17(14): 3925-9, 2007 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-17531479

RESUMEN

Structure-activity relationships and efforts to optimize the pharmacokinetic profile of a class of 2-arylimino-5,6-dihydro-4H-1,3-thiazines as cannabinoid receptor agonists are described. Among the compounds examined, compound 14 showed potent affinity and high selectivity for CB2, and compound 23 showed potent affinities against CB1 and CB2. These compounds displayed oral bioavailability.


Asunto(s)
Agonistas de Receptores de Cannabinoides , Tiazinas/farmacología , Administración Oral , Disponibilidad Biológica , Tiazinas/administración & dosificación , Tiazinas/farmacocinética
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