1.
Bioorg Med Chem Lett
; 13(22): 4059-63, 2003 Nov 17.
Artículo
en Inglés
| MEDLINE
| ID: mdl-14592508
RESUMEN
Tetrapeptide-based peptidomimetic compounds have been shown to effectively inhibit the hepatitis C virus NS3.4A protease without the need of a charged functionality. An aldehyde is used as a prototype reversible electrophilic warhead. The SAR of the P1 and P2 inhibitor positions is discussed.
Asunto(s)
Hepacivirus/enzimología , Oligopéptidos/síntesis química , Oligopéptidos/farmacología , Inhibidores de Proteasas/síntesis química , Hepacivirus/efectos de los fármacos , Cinética , Modelos Moleculares , Inhibidores de Proteasas/farmacología , Conformación Proteica , Relación Estructura-Actividad , Difracción de Rayos X
2.
Bioorg Med Chem Lett
; 14(6): 1441-6, 2004 Mar 22.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15006379
RESUMEN
The alpha-ketoamide warhead (e.g., 15) was found to be a practical replacement for aliphatic aldehydes in a series of HCV NS3.4A protease inhibitors. Structure-activity relationships and prime side optimization are discussed.