1.
J Med Chem
; 62(3): 1348-1361, 2019 02 14.
Artigo
em Inglês
| MEDLINE
| ID: mdl-30609350
RESUMO
A series of 5,6,7,8-tetrahydro-1,6-naphthyridine derivatives targeting the allosteric lens-epithelium-derived-growth-factor-p75 (LEDGF/p75)-binding site on HIV-1 integrase, an attractive target for antiviral chemotherapy, was prepared and screened for activity against HIV-1 infection in cell culture. Small molecules that bind within the LEDGF/p75-binding site promote aberrant multimerization of the integrase enzyme and are of significant interest as HIV-1-replication inhibitors. Structure-activity-relationship studies and rat pharmacokinetic studies of lead compounds are presented.
Assuntos
Inibidores de Integrase de HIV/farmacologia , HIV-1/efeitos dos fármacos , Naftiridinas/farmacologia , Sítio Alostérico , Cristalografia por Raios X , Infecções por HIV/tratamento farmacológico , Inibidores de Integrase de HIV/química , Inibidores de Integrase de HIV/uso terapêutico , HIV-1/enzimologia , HIV-1/fisiologia , Humanos , Naftiridinas/química , Naftiridinas/uso terapêutico , Replicação Viral/efeitos dos fármacos
2.
Manag Care
; 19(7): 33-5, 2010 Jul.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20672529