抗血吸虫病药物的研究——S-(5-硝基呋喃-2-甲酰)-缩氨基硫脲类及有关化合物的合成

本文报导S-(5-硝基呋喃-2-甲酰)-缩氨基硫脲类和S-(5-硝基呋喃-2-甲酰)-取代缩氨基硫脲类、次烷烃基-双-S-(5-硝基呋喃-2-甲酰)]-缩氨基硫脲和次苯基-双-S-(5-硝基呋喃-2-甲酰)]-缩氨基硫脲类等31个化合物的合成.经日本血吸虫病动物筛选试验,发现S-(5-硝基呋喃-2-甲酰)丙酮-苄基取代缩氨基硫脲(Ⅳ)和S-(5-硝基呋喃-2-甲酰)-了酮-缩氨基硫脲(Ⅺ)给二组病鼠治疗后检获虫数比对照组鼠有所减少.

STUDIES ON ANTIBILHARZIAL DRUGS SYNTHESIS OF S-(5-NITRO-2-FUROYL)-THIOSEMICARBAZONES AND RELATED COMPOUNDS

S-(5-nitro-2-furoyl)thiosemicarbazones and S- (5-nitro-2-furoyl) -substituted thiosemi- carbazones were prepared by reaction of 5-nitro-2-furoyl chloride with thiosemicarbazide or substituted thiosemicarbazides in dry acetone, or with thiosemica rbazones in dry tetra- hydrofuran in the presence of sodium bicarbonate. Similarly, alkylene-bis -S- (5-nitro-2- furoyl)]-thiosemicarbazones and phenylene-bis--S-(5-nitro-2-furoyl)]-thiosemicarbazones were prepared by using two equivalent weight of 5-nitro-2-furoyl chloride. The resulted compounds were screened in mice against schistosomiasis japonica. The results indicated that two compounds, S- (5-nitro-2-furoyl) -acetone-benzyl-thiosemicarbazone (Ⅳ) and S- (5-nitro-2-furoyl) -butanone-thiosemicarbazone (Ⅺ), possessed some chemoprophylactic activity.