pyrazofurin and mizoribine

The recent progress in antiviral chemotherapy against respiratory syncytial virus (RSV) infections was reviewed. RSV infections among high risk individuals, such as premature babies, infants with congenital disease of cardiopulmonary system or immune system and the aged, hospitalised patients with immunosuppressed status are threatened, with high mortality rates and thus need anti-viral chemotherapy. Clinical efficacy of ribavirin and humanized monoclonal antibody (mAb) against RSV infections as well as experimental reports of novel anti-RSV compounds under investigation such as membrane fusion inhibitors were introduced.

Topics: Amides; Animals; Antibodies, Monoclonal; Antiviral Agents; Biopolymers; Bridged-Ring Compounds; Catechin; Drugs, Investigational; Heterocyclic Compounds; Humans; Immunoglobulins, Intravenous; Lipids; N-Acetylneuraminic Acid; Norbornanes; Oligodeoxyribonucleotides, Antisense; Pyrazoles; Respiratory Syncytial Virus Infections; Respiratory Syncytial Viruses; Ribavirin; Ribonucleosides; Ribose; Risk Factors; Thiocarbamates; Thiones

5-Hydroxy-1-(beta-D-ribofuranosyl)-1,2,3-triazole-4-carboxamide (II) has been prepared by direct glycosylation of the trimethylsilyl derivative of 5-hydroxy-1,2,3-triazole-4-carboxamide (IV). The use of trimethylsilyltrifluoromethane sulfonate as a catalyst and 1-O-acetyl-2,3,5-tri-O-benzoyl-beta-D-ribofuranose in acetonitrile gave a 95% yield of a 1:1 mixture of V and VI as blocked nucleosides which were readily separated on a silica gel column. The synthesis of II was also achieved by the cycloaddition of 2,3,5-tri-O-benzoyl-beta-D-ribofuranosyl azide with ethyl malonamate. II shows significant antiviral activity against herpes and measles virus in vitro.

Topics: Amides; Animals; Carcinoma, Ehrlich Tumor; Drug Evaluation, Preclinical; IMP Dehydrogenase; Mice; Nucleosides; Pyrazoles; Ribonucleosides; Ribose; Structure-Activity Relationship; Triazoles