Respiratory syncytial virus fusion inhibitors. Part 4: optimization for oral bioavailability.
Bioorg Med Chem Lett
; 17(4): 895-901, 2007 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-17169560
ABSTRACT
A series of benzimidazole-based inhibitors of respiratory syncytial virus (RSV) fusion were optimized for antiviral potency, membrane permeability and metabolic stability in human liver microsomes. 1-Cyclopropyl-1,3-dihydro-3-[[1-(4-hydroxybutyl)-1H-benzimidazol-2-yl]methyl]-2H-imidazo[4,5-c]pyridin-2-one (6m, BMS-433771) was identified as a potent RSV inhibitor demonstrating good bioavailability in the mouse, rat, dog and cynomolgus monkey that demonstrated antiviral activity in the BALB/c and cotton rat models of infection following oral administration.
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Base de dados:
MEDLINE
Assunto principal:
Antivirais
/
Benzimidazóis
/
Vírus Sincicial Respiratório Humano
Idioma:
En
Ano de publicação:
2007
Tipo de documento:
Article