1.
Bioorg Med Chem Lett
; 17(5): 1392-8, 2007 Mar 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17194584
RESUMO
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.
Assuntos
Inibidores de Integrase de HIV/síntese química , Inibidores de Integrase de HIV/farmacocinética , Naftiridinas/síntese química , Administração Oral , Animais , Células Cultivadas , Integrase de HIV/efeitos dos fármacos , Integrase de HIV/genética , Inibidores de Integrase de HIV/farmacologia , Humanos , Concentração Inibidora 50 , Mutação , Naftiridinas/farmacocinética , Naftiridinas/farmacologia , Ratos , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 16(11): 2900-4, 2006 Jun 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16554152
RESUMO
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.
