1.
Bioorg Med Chem Lett
; 13(4): 697-700, 2003 Feb 24.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12639561
RESUMO
A novel series of benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 31 is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects.
Assuntos
Benzamidinas/farmacologia , Receptores de N-Metil-D-Aspartato/antagonistas & inibidores , Administração Oral , Animais , Benzamidinas/síntese química , Carragenina , Avaliação Pré-Clínica de Medicamentos , Hiperalgesia/tratamento farmacológico , Dor/tratamento farmacológico , Desempenho Psicomotor/efeitos dos fármacos , Ratos , Relação Estrutura-Atividade
2.
J Med Chem
; 46(4): 453-6, 2003 Feb 13.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12570367
RESUMO
Naphthyridine 7 inhibits the strand transfer of the integration process catalyzed by integrase with an IC50 of 10 nM and inhibits 95% of the spread of HIV-1 infection in cell culture at 0.39 microM. It does not exhibit cytotoxicity in cell culture at < or =12.5 microM and shows a good pharmacokinetic profile when dosed orally to rats. The antiviral activity of 7 and its effect on integration were confirmed using viruses with specific integrase mutations.