SYNTHESIS OF NEW ANTISCHISTOSOMAL AGENTS RELATED TO FUVINAZOLE

Several series of nitrofuranvinyloxadiazoles related to fuvinazole, a new antischistosomal drug, were synthesized by using β-(5-nitro-furyl) acrylamide oxime as the starting material. Another series of nitrofuranoxadiazole compounds without vinyl bridge was also synthesized by using 5-nitro-2-furamidoxime as starting material in order to investigate the significance of the presence of vinyl bridge. The synthesized compounds were screened against schistosomiasis japonica in mice. The results showed that the presence of 5-acylamino group or 5-alkylaminomethyl group on the oxadiazole ring afforded optimal potency and that desvinyl analogs were almost inactive. The structure-activity relationship was discussed.