| Literature DB >> 17169560 |
Kuo-Long Yu1, Ny Sin, Rita L Civiello, X Alan Wang, Keith D Combrink, H Belgin Gulgeze, Brian L Venables, J J Kim Wright, Richard A Dalterio, Lisa Zadjura, Anthony Marino, Sandra Dando, Celia D'Arienzo, Kathleen F Kadow, Christopher W Cianci, Zhufang Li, Junius Clarke, Eugene V Genovesi, Ivette Medina, Lucinda Lamb, Richard J Colonno, Zheng Yang, Mark Krystal, Nicholas A Meanwell.
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.Entities:
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Year: 2006 PMID： 17169560 DOI： 10.1016/j.bmcl.2006.11.063
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823