Discovery of ANA975: An Oral Prodrug of the TLR-7 Agonist Isatoribine.

Autor:	Xiang, AlanX., Webber, StephenE., Kerr, BradleyM., Rueden, ErikJ., Lennox, JosephR., Haley, GregoryJ., Wang, Tingmin, Ng, JohnS., Herbert, MarkR., Clark, DavidL., Banh, VirginiaN., Li, Wei, Fletcher, SimonP., Steffy, KevinR., Bartkowski, DarianM., Kirkovsky, LeonidI., Bauman, LisaA., Averett, DevronR.
Předmět:	NUCLEOSIDES HEPATITIS C virus PRODRUGS NUCLEOTIDES HEPATITIS viruses
Zdroj:	Nucleosides, Nucleotides & Nucleic Acids; Jun2007, Vol. 26 Issue 6/7, p635-640, 6p, 3 Diagrams, 2 Graphs
Abstrakt:	ANA975, a 5-amino-3-β -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. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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