1199809-32-9Relevant articles and documents
The synthesis of hydroxyaminopurine nucleosied (by machine translation)
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, (2016/10/10)
A compound or salt thereof having the following structure useful for the treatment of hepatitis C virus (HCV): wherein R 7 is C 1-6 alkyl or C 3-6 cycloalkyl and R 8 is -O(C 1-6 alkyl) or -O(C 3-6 cycloalkyl).
2′-Deoxy-2′-α-fluoro-2′-β-C-methyl 3′,5′-cyclic phosphate nucleotide prodrug analogs as inhibitors of HCV NS5B polymerase: Discovery of PSI-352938
Reddy, P. Ganapati,Bao, Donghui,Chang, Wonsuk,Chun, Byoung-Kwon,Du, Jinfa,Nagarathnam, Dhanapalan,Rachakonda, Suguna,Ross, Bruce S.,Zhang, Hai-Ren,Bansal, Shalini,Espiritu, Christine L.,Keilman, Meg,Lam, Angela M.,Niu, Congrong,Steuer, Holly Micolochick,Furman, Phillip A.,Otto, Michael J.,Sofia, Michael J.
scheme or table, p. 7376 - 7380 (2011/02/28)
A series of novel 2′-deoxy-2′-α-fluoro-2′-β-C- methyl 3′,5′-cyclic phosphate nucleotide prodrug analogs were synthesized and evaluated for their in vitro anti-HCV activity and safety. These prodrugs demonstrated a 10-100-fold greater potency than the parent nucleoside in a cell-based replicon assay due to higher cellular triphosphate levels. Our structure-activity relationship (SAR) studies provided compounds that gave high levels of active triphosphate in rat liver when administered orally to rats. These studies ultimately led to the selection of the clinical development candidate 24a (PSI-352938).