The most promising compound, namely the O-[S-(hydroxyl)pivaloyl-2-thioethyl]{abbreviated as O-[(HO)tBuSATE)]} N-benzylamine phosphoramidate diester derivative (IDX184), was selected for further in vivo studies, and was the first clinical pronucleotide evaluated for the treatment of chronic hepatitis C up to Phase II trials.
As part of our anti-hepatitis C program, we recently discovered 2'-C-methylcytidine (1) and 2'-C-methyluridine (2), which are potent inhibitors in cell culture of several viruses (bovine viral diarrhea virus (BVDV), yellow fever virus (YFV)) closely related to HCV. In order to characterize structure-activity relationships, we introduced some structural and functional modifications into the 3'-position of 2'-C-methylcytidine and 2'-C-methyluridine. All these hitherto unknown compounds thus synthesized were tested for the activity against a wide range of viruses and found to be inactive.
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