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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Yu KL,Sin N,Civiello RL,Wang XA,Combrink KD,Gulgeze HB,Venables BL,Wright JJ,Dalterio RA,Zadjura L,Marino A,Dando S,D'Arienzo C,Kadow KF,Cianci CW,Li Z,Clarke J,Genovesi EV,Medina I,Lamb L,Colonno RJ,Yang Z,Kr

doi

10.1016/j.bmcl.2006.11.063

subject

Has Abstract

pub_date

2007-02-15 00:00:00

pages

895-901

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)01358-8

journal_volume

17

pub_type

杂志文章

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