Chemotherapeutic nitroheterocycles. Antischistosomal properties of nitrofurylvinyl and nitrothienylvinyl heterocycles

Article abstract of DOI:10.1021/jm00269a015

A series of 24 analogs of the experimental antischistosomal agent, 5 amino 3 [2 (5 nitro 2 furyl) vinyl] 1,2,4 oxadiazole, was prepared and evaluated in mice infected with Schistosoma mansoni. Although antischistosomal activity was widespread in the series, only four of the compounds showed significant curative properties. Compounds containing 2 imidazolyl and 2 pyridyl groups gave cure rates around 25% at 400 and 250 mg/kg dose levels, respectively. The 2 thiazolyl and 2 pyrimidyl derivatives were especially notable, yielding 100% cures at 250 and 200 mg/kg dose levels, respectively.