期刊
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
卷 26, 期 6-7, 页码 635-640出版社
TAYLOR & FRANCIS INC
DOI: 10.1080/15257770701490472
关键词
ANA975; isatoribine; prodrug; nucleoside; hepatitis C; toll-like receptor
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 ANA 975. 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.
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