Portal de Periódicos da CAPES

Respiratory syncytial virus fusion inhibitors. Part 4: Optimization for oral bioavailability

2006; Elsevier BV; Volume: 17; Issue: 4 Linguagem: Inglês

10.1016/j.bmcl.2006.11.063

1464-3405

Kuo‐Long Yu, Ny Sin, Rita L. Civiello, X. Alan Wang, Keith D. Combrink, H. Belgin Gülgeze, Brian L. Venables, J. J. Wright, R. A. Dalterio, Lisa Zadjura, Anthony M. Marino, Sandra A. Dando, Celia D’Arienzo, Kathleen F. Kadow, Christopher Cianci, Zhufang Li, Junius Clarke, Eugene V. Genovesi, Ivette Medina, Lucinda Lamb, Richard J. Colonno, Yang Zheng, Mark Krystal, Nicholas A. Meanwell,

Influenza Virus Research Studies

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.