| Literature DB >> 18066870 |
Alan X Xiang1, Stephen E Webber, Bradley M Kerr, Erik J Rueden, Joseph R Lennox, Gregory J Haley, Tingmin Wang, John S Ng, Mark R Herbert, David L Clark, Virginia N Banh, Wei Li, Simon P Fletcher, Kevin R Steffy, Darian M Bartkowski, Leonid I Kirkovsky, Lisa A Bauman, Devron R Averett.
Abstract
ANA975, a 5-amino-3-beta -D-ribofuranosyl-3H-thiazolo[4,5-d]pyrimidin-2-one derivative, was synthesized in the search of an oral prodrug of isatoribine, a small molecule toll-like receptor 7 (TLR-7) agonist. Several strategies were studied to enable the kilogram-scale synthesis of ANA975. Three general total syntheses are described. In the phase I clinical study of ANA975 against hepatitis C virus (HCV), conversion to isatoribine in plasma was rapid and effective, delivering levels of isatoribine that have been shown to be clinically relevant.Entities:
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Year: 2007 PMID： 18066870 DOI： 10.1080/15257770701490472
Source DB: PubMed Journal: Nucleosides Nucleotides Nucleic Acids ISSN： 1525-7770 Impact factor: 1.381