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Synthesis of 9-(2-beta-C-methyl-beta-d-ribofuranosyl)-6-substituted purine derivatives as inhibitors of HCV RNA replication. 2005
Yili Ding, and
Jean-Luc Girardet, and
Zhi Hong, and
Vicky C H Lai, and
Haoyun An, and
Yung-Hyo Koh, and
Stephanie Z Shaw, and
Weidong Zhong
Valeant Pharmaceuticals International, 3300 Hyland Avenue Costa Mesa, CA 92626, USA. yding@icnpharm.com
A series of 9-(2'-beta-C-methyl-beta-d-ribofuranosyl)-6-substituted purine derivatives were synthesized as potential inhibitors of HCV RNA replication. Their inhibitory activities in a cell based HCV replicon assay were reported. A prodrug approach was used to further improve the potency of these compounds by increasing the intracellular levels of 5'-monophosphate metabolites. These nucleotide prodrugs showed much improved inhibitory activities of HCV RNA replication.
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