Abuzar S, Sharma S, Visen P K, Gupta S, Katiyar J C
Arzneimittelforschung. 1986 Mar;36(3):416-9. doi: 10.1002/chin.198630211.
A number of substituted diphenylsulfides and sulfones (4-11) and 2,2'-disubstituted-5,5'-dibenzimidazolyl sulfides and sulphones (12-19) have been synthesized starting from 5-chloro-2-nitroacetanilide and (3) 4,4'-dichlorodiphenyl sulfone (9), respectively. Among the compounds tested against Ancylostoma ceylanicum in hamsters and Hymenolepis nana in rats and mice, 14, 15, 18 and 19 removed 100% of the worms at an oral dose of 25 mg/kg X 1 to 250 mg/kg X 3. Some of the compounds were tested for their blood schizontocidal activity against Plasmodium berghei in mice but none showed any activity up to an oral dose of 10 mg/kg given for 6 days.
分别从5-氯-2-硝基乙酰苯胺和4,4'-二氯二苯砜（9）出发，合成了一系列取代二苯硫醚和砜（4-11）以及2,2'-二取代-5,5'-二苯并咪唑基硫醚和砜（12-19）。在针对仓鼠体内的锡兰钩虫以及大鼠和小鼠体内的微小膜壳绦虫进行测试的化合物中，化合物14、15、18和19在口服剂量为25mg/kg×1至250mg/kg×3时可清除100%的蠕虫。部分化合物针对小鼠体内的伯氏疟原虫进行了血裂殖体杀灭活性测试，但在口服剂量为10mg/kg、连续给药6天的情况下，均未显示出任何活性。
