申请人:ICN Pharmaceuticals, Inc.
公开号:US03968103A1
公开(公告)日:1976-07-06
Novel substituted 1,2,3-triazole nucleosides such as 4-R'-2-.beta.-D-ribofuranosyl-1,2,3-triazole wherein R' is a nitro, carboxylic acid ester, cyano, carboxamide or thiocarboxamide group are prepared by a procedure entailing fusion of an appropriately substituted 1,2,3-triazole with a tetra-0-acyl blocked ribofuranose. The resulting compounds exhibit significant antimicrobial activity in in vitro testing or are useful in preparing compounds which exhibit such activity.
本发明提供了一种新型的替代1,2,3-三唑核苷类化合物,例如4-R'-2-.beta.-D-核糖呋喃基-1,2,3-三唑,其中R'为硝基、羧酸酯、氰基、羧酰胺或硫代羧酰胺基团。该化合物的制备方法包括将适当取代的1,2,3-三唑与四个O-酰基阻滞的核糖呋喃糖融合。所得化合物在体外测试中表现出显著的抗微生物活性,或可用于制备表现出此类活性的化合物。