Design, synthesis and biological evaluation of 2 '-deoxy-2 ',2 '-difluoro-5-halouridine phosphoramidate ProTides

作者：Quintiliani Maurizio; Persoons Leentje; Solaroli Nicola; Karlsson Anna; Andrei Graciela; Snoeck Robert; Balzarini Jan; McGuigan Christopher^*

来源：Bioorganic & Medicinal Chemistry, 2011, 19(14): 4338-4345.

DOI：10.1016/j.bmc.2011.05.037

• Antiviral
• Herpes virus
• Feline herpes
• Nucleoside
• Nucleotide
• ProTide
• Phosphoramidate
• Pro-drug

We report the synthesis of a series of novel 2'-deoxy-2',2'-difluoro-5-halouridines and their corresponding phosphoramidate ProTides. All compounds were evaluated for antiviral activity and for cellular toxicity. Interestingly, 2'-deoxy-2',2'-difluoro-5-iodo- and -5-bromo-uridines showed selective activity against feline herpes virus replication in cell culture due to a specific recognition (activation) by the virus-encoded thymidine kinase.

• 出版日期2011-7-15