1.
Bioorg Med Chem Lett
; 17(5): 1392-8, 2007 Mar 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17194584
RESUMEN
A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent ability to inhibit virus with mutant enzyme.
Asunto(s)
Inhibidores de Integrasa VIH/síntesis química , Inhibidores de Integrasa VIH/farmacocinética , Naftiridinas/síntesis química , Administración Oral , Animales , Células Cultivadas , Integrasa de VIH/efectos de los fármacos , Integrasa de VIH/genética , Inhibidores de Integrasa VIH/farmacología , Humanos , Concentración 50 Inhibidora , Mutación , Naftiridinas/farmacocinética , Naftiridinas/farmacología , Ratas , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 16(11): 2900-4, 2006 Jun 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16554152
RESUMEN
A series of 5-amino derivatives of 8-hydroxy[1,6]-naphthyridine-7-carboxamide exhibiting sub-micromolar potency against replication of HIV-1 in cell culture was identified. One of these analogs, compound 12, displayed excellent pharmacokinetic properties when dosed orally in rats and in monkeys. This compound was demonstrated to be efficacious against replication of simian-human immunodeficiency virus (SHIV) 89.6P in infected rhesus macaques.