MODIFIED BENZIMIDAZOLE NUCLEOSIDES AS ANTIVIRAL AGENTS

摘要

This invention pertains to nucleoside analogs which have antiviral activity and improved metabolic stability. More specifically, this invention pertains to modified sugar benzimidazole nucleosides, as exemplified by compounds such as benzimidazole nucleosides possessing a fluorinated sugar-like moiety (for example, a 2'-fluoro-furanosyl moiety or a 3'-fluoro-furanosyl moiety), and may be represented by formula (I) wherein R1 is a fluorinated sugar-like moiety; and R?2, R4, R5, R6 and R7¿ are benzimidazole substituents, such as -H, halogens (e.g., -F, -C1, -Br, -I), -NO¿2?, -NR2 (where R is independently -H or an alkyl group having 1-6 carbon atoms), -OR (where R is -H or an alkyl group having 1-6 carbon atoms), -SR (where R is -H or a hydrocarbyl of 1-10 carbon atoms), and -CF3. In one embodiment, R?1¿ is 2'-fluoro-furanosyl or 3'-fluoro-furanosyl; R2 is -H, -F, -C1, -Br, -I, or -NR¿2?, wherein R is independently -H or an alkyl group having 1-6 carbon atoms; R?4, R5, R6 and R7¿ are independently -H, -F, -C1, -Br, or -I.