The Synthesis and Study of New Ribavirin Derivatives and Related Nucleoside Azole Carboxamides as Agents Active against RNA Viruses.

摘要

To examine the structural parameters necessary for antiviral efficacy of certain azole carboxamide nucleosides and nucleotides, several imidazole, pyrazole and 1,2,4-triazole carboxamide nucleosides have been synthesized. New methods have been developed to prepare Ribavirin derivatives. All the compounds prepared during the subject contract have been tested at the U.S. Army Medical Research Institute of Infectious Diseases, Fort Detrick. Ribavirin 3',5'-cyclic phosphate (BJ-58536) exhibited superior in vivo activity against Venezuelan equine encephalitis (VEE) over that of ribavirin. In preliminary results on day 20 at 25 mg/kg/day of BJ-58536 there were 20 out of 20 survivors in the VEE-infected mice compared to 8 out of 20 survivors in the control. (Author)