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Bioorg Med Chem Lett. 2007 Feb 15;17(4):895-901. Epub 2006 Dec 1.

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

Author information

1
Department of Chemistry, The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA.

Erratum in

  • Bioorg Med Chem Lett. 2007 Apr 15;17(8):2385.

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.

PMID:
17169560
DOI:
10.1016/j.bmcl.2006.11.063
[Indexed for MEDLINE]

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