5-HALOGENO-3'-FLUORO-2',3'-DIDEOXYURIDINE COMPOUNDS AND THEIR THERAPEUTIC APPLICATION

摘要

The novel 5-halogeno-3'-fluoro-2',3'-dideoxyuridines particularly FddClUrd, FddBrUrd, FddIUrd and FddFUrd proved antivirally effective in several in vitro systems (i.e. HIV-1 replication in MT4 and HUT-78 cells and HIV-2 replication in MT4 cells). Of these FddUrd derivatives FddClUrd is endowed with the highest selectivity index in vitro, comparable to that AzddThd in MT4 cells. These observations make the members of the 5-halogeno-substituted FddUrd derivatives attractive antivirals agents for the treatment of AIDS, AIDS-related diseases and retroviral diseases including hepatitis B.