Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus.

Christopher McGuigan,Karolina Madela,Mohamed Aljarah,Arnaud Gilles,Andrea Brancale,Nicola Zonta,Stanley Chamberlain,John Vernachio,Jeff Hutchins,Andrea Hall,Brenda Ames,Elena Gorovits,Babita Ganguly,Alexander Kolykhalov,Jin Wang,Jerry Muhammad,Joseph M Patti,Geoffrey Henson

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

Phosphoramidate ProTides of 2′-C-Me-6-MeOG are up to 500-fold more potent versus HCV than the 2′-C-MeG parent, being active at nanomolar levels. The lead has entered phase 1 clinical trials for HCV.

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关键词

HCV,ProTide,Phosphoramidate,Nucleoside,Nucleotide,Antiviral pro-drug,Polymerase,NS5B

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