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鉴于2,2＇-二羟基-3,3＇-二溴代-5,5＇-二氯代二苯硫醚(I_a,抗虫349)与2,2＇-二羟基-3,3＇,5,5＇,6,6＇-六氯代二苯硫醚(I_b抗虫390)对小白鼠体内的日本血吸虫具有明显的抑制与杀灭作用,乃合成一系列有关化合物。亚砜化合物(II_a、II_b)系由相应的硫醚(I_a、I_b)在冰醋酸中用过氧化氢氧化制成。2,2＇-二羟基-4,4＇,5,5＇-四氯代二苯硫醚(I_d)用溴素溴化得化合物I_c。化合物I_(d-f)系由苯环上带有相应取代基的苯酚与二氯化硫缩合而得。化合物I_(g-o)系由对位带有各种不同基因(Cl、Br、CH_3等)的2,2＇-二羟基二苯硫醚、甲醛与相应的仲胺在乙醇中进行Mannich反应而得。化合物I_a、I_b溶于苯中与无水(?)(?)嗪苯溶液作用分别得相应的(?)(?)嗪盐。动物试验结果指出2,2＇-二羟基-3,3＇-二溴代-4,4＇,5,5＇-四氯代二苯硫醚(I_c,编号抗虫438)、2,2＇-二羟基-3,3＇-二溴代-5,5＇-二氯代二苯亚砜(II_a,编号抗虫436)、2,2＇-二羟基-3,3＇,5,5＇,6,6＇-六氯代二苯亚砜(II_b,编号抗虫422)、以及2,2＇-二羟基-3,3＇-二溴代-5,5＇-二氯代二苯硫醚、2,2＇-二羟基-3,3＇,5,5＇,6,6＇-六氯代二苯硫醚的(?)(?)嗪盐对小白鼠体内的日本血吸虫均有明显的抑制与杀灭作用,详细的药理结果将另文报导。
In view of the fact that 2,2’-dihydroxy-3,3’-dibromo-5,5’-dichlorodiphenyl sulfide (I_a, Insect Resistant 349) , 5,5 ’, 6,6’-hexachlorodiphenyl sulfide (I_b insect 390) on mice Schistosoma japonicum significantly inhibited and killed, but the synthesis of a series of related compounds. The sulfoxide compounds (II_a, II_b) were prepared from the corresponding thioethers (I_a, I_b) by oxidation with hydrogen peroxide in glacial acetic acid. 2,2’-Dihydroxy-4,4 ’, 5,5’-tetrachlorodiphenyl sulfide (I_d) was brominated with bromine to give compound I_c. Compound I_ (d-f) is derived from the condensation of benzene with sulfur dichloride and the corresponding substituent on benzene ring. The compound I_ (go) consists of 2,2’-dihydroxydiphenyl sulfide para-position with various genes (Cl, Br, CH_3, etc.) and Mannich reaction of formaldehyde with the corresponding secondary amine in ethanol . Compounds I_a and I_b were dissolved in benzene and reacted with anhydrous (?) - oxazine solution respectively to give the corresponding (?)?? Animal test results indicate that 2,2’-dihydroxy-3,3’-dibromo-4,4 ’, 5,5’-tetrachlorodiphenyl sulfide (I_c, ’-dihydroxy-3,3’-dibromo-5,5’-dichlorobiphenyl sulfoxide (II_a, code ID 436), 2,2’-dihydroxy-3,3’ 5 ’, 6,6’-hexachlorodiphenyl sulfoxide (II_b, numbered insecticide 422) and 2,2’-dihydroxy-3,3’-dibromo-5,5’-dichloro Diphenyl sulfide, (?) (+) - (4-oxazinyl) 2,2’-dihydroxy-3,3 ’, 5,5’, 6,6’-hexachlorodiphenyl sulfide in Japan Schistosoma have significant inhibitory and killing effect, the detailed pharmacological results will be reported in another article.