1.
Bioorg Med Chem Lett
; 19(17): 5246-9, 2009 Sep 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-19620004
RESUMEN
A series of piperazine derivatives were designed and synthesised as gp120-CD4 inhibitors. SAR studies led to the discovery of potent inhibitors in a cell based anti viral assay represented by compounds 9 and 28. The rat pharmacokinetic and antiviral profiles of selected compounds are also presented.
Asunto(s)
Antígenos CD4/metabolismo , Proteína gp120 de Envoltorio del VIH/antagonistas & inhibidores , Inhibidores de Fusión de VIH/química , Piperazinas/química , Animales , Disponibilidad Biológica , Línea Celular Tumoral , Diseño de Fármacos , Proteína gp120 de Envoltorio del VIH/metabolismo , Inhibidores de Fusión de VIH/síntesis química , Inhibidores de Fusión de VIH/farmacocinética , VIH-1/efectos de los fármacos , Humanos , Microsomas Hepáticos/metabolismo , Piperazinas/síntesis química , Piperazinas/farmacocinética , Ratas , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 19(17): 5250-5, 2009 Sep 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-19632839
RESUMEN
The synthesis and structure-activity relationship of a series of novel gp120-CD4 inhibitors are described. Pharmacokinetic studies and antiviral spectrum assessment of lead compounds led to the identification of compound 36, a potent gp120-CD4 inhibitor which exhibited antiviral potency across a spectrum of 25 clade B isolates.