Zenkov N K, Men'shchikova E B, Kandalintseva N V, Prosenko A E
Research Center of Clinical and Experimental Medicine, Siberian Division of the Russian Academy of Medical Sciences, Novosibirsk, Russia.
Bull Exp Biol Med. 2009 May;147(5):592-5. doi: 10.1007/s10517-009-0574-3.
Structurally related phenols containing the p-alkylthiosulfonate substituent and partially hindered by tert-butyl groups were synthesized for the search and development of new synthetic antioxidant, which would be effective in vivo in preventing free radical-induced pathological processes. Sodium 3-(3'-tert-butyl-4'-hydroxyphenyl)propylthiosulfonate had high antiinflammatory activity and produced a dose-dependent effect (IC(50)=36 mg/kg). Changes in the length of the carbohydrate chain in the p-alkyl substituent had no effect on in vitro antiradical activity of the test compounds. However, the decrease in the length of this chain by one methylene unit was accompanied by reduction of antiinflammatory activity of the end product. Lengthening of the chain did not modulate these properties.
为了寻找和开发新型合成抗氧化剂，合成了含有对烷基硫代磺酸酯取代基且部分被叔丁基阻碍的结构相关酚类化合物，这类抗氧化剂在体内预防自由基诱导的病理过程方面应具有有效性。3-(3'-叔丁基-4'-羟基苯基)丙基硫代磺酸钠具有高抗炎活性，并呈现剂量依赖性效应（半数抑制浓度=36毫克/千克）。对烷基取代基中碳水化合物链长度的改变对测试化合物的体外抗自由基活性没有影响。然而，该链长度减少一个亚甲基单元会伴随着最终产物抗炎活性的降低。链的延长并未调节这些性质。
