| Title | Synthesis and antiviral acticity of some phosphates of the broad-spectrum antiviral nucleoside, 1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide (ribavirin). | ||
| Author | Allen, L B; Boswell, K H; Khwaja, T A; Meyer, R B Jr; Sidwell, R W; Witkowski, J T; Christensen, L F; Robins, R K | ||
| Journal | J Med Chem | Publication Year/Month | 1978-Aug |
| PMID | 211234 | PMCID | -N/A- |
1-beta-D-Ribofuranosyl-1,2,4-triazole-3-carboxamide 5\'-phosphate (2) was prepared and converted into the following derivatives: the 5\'-phosphoramidate 3, the 5\'-diphosphate 4, the 5\'-triphosphate 5, and the cyclic 3\',5\'-phosphate 6. The cyclic 2\',3\'-phosphate 7 was prepared from the parent nucleoside, 1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide (1), and was opened to the 2\'(3\')-phosphate 8. These compounds were found to exhibit significant antiviral activity against several viruses in cell culture. Ribavirin 5\'-phosphate (2) was shown to be effective when tested against lethal infections in mice caused by influenza A2, influenza B, and murine hepatitis viruses.