Synthesis, structure, and antiparasitic activity of sulfamoyl derivatives of ribavirin

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Abstract
The triazole nucleoside derivatives 1-(5''-O-sulfamoyl-.beta.-D-ribofuranosyl) [1,2,4]triazole-3-carboxamide (2), 1-(5''O-sulfamoyl-.beta.-D-ribofuranosyl)[1,2,4]triazole-3-thiocarboxamide (3), and 1-(5''-O-sulfamoyl-.beta.-D-ribofuranosyl)-[1,2,4]triazole-3-carbonitrile (4) were synthesized. Suitably protected triazole nucleosides were converted to their corresponding 5''-sulfamoyl derivatives, which on subsequent deprotection gave the desired compounds in good yields. The structures of compounds 2-4 were confirmed by X-ray crystallographic analysis. All three compounds showed significant antiparasitic activity in vitro, while 2 showed significant activity in vivo against Leishmania donovani and Trypanosoma brucei.
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