| Autor: |
Gabrielsen, B., Kirsi, J. J., Kwong, C. D., Carter, D. A., Krauth, C. A., Hanna, L. K., Huggins, J. W., Monath, T. P., Kefauver, D. F., Blough, H. A., Rankin, J. T., Bartz, C. M., Huffman, J. H., Smee, D. F., Sidwell, R. W., Shannon, W. M., Secrist, J. A. |
| Zdroj: |
Antiviral Chemistry & Chemotherapy; August 1994, Vol. 5 Issue: 4 p209-220, 12p |
| Abstrakt: |
A series of 29 pyrimidines comprising analogues of 6-azauridine (e.g. 2- and 4-thio-6-azauridine), 6-substituted uridines (including several known inhibitors of orotidine 5′-monophosphate decarboxylase, ODCase, e.g. pyrazofurin), and 6-azauridine-5′-(ethyl methoxyalaninyl) phosphate (a potential prodrug of 6-AU-5′-MP) were synthesized and evaluated in vitroand in vivoagainst five RNA viruses: Japanese encephalitis (JE), yellow fever (YF), sandfly fever (SF), Punta Tora (PT) and Venezuelan equine encephalomyelitis (VEE) viruses. 2-Thio-6-azauridine demonstrated the best In vitroactivity against all five viruses. However, in vivoactivity was not observed in JE-, PT- and VEE-infected mice. The phosphate prodrug of 6-azauridine was significantly more effective than the parent compound in the PT virus mouse model. Optimum in vivodose/route/schedule was determined for pyrazofurin in PT-virus-infected mice. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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