抗血吸虫药茚满酮类及萘满酮类化合物的合成
SYNTHESIS OF INDANONES AND TETRALONES AS NEW POTENTIAL SCHISTOSOMICIDALS
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摘要: 取代水杨酰胺类化合物(包括氯硝柳胺)对动物日本血吸虫病有预防和治疗作用。取代茚满类化合物的结构与取代水杨酰胺类有相似之处。据此,合成了各种取代茚满酮类化合物91个,有效者为23个,其中以化合物8,15(S 72059),18,30,76效果较显著。有效化合物均具有酮肟结构,其药效专属性较为明显。Abstract: In view of the fact that the structure of substituted indanones possesses some similarity to the substituted salicylamides which have been shown to be active against schistosomiasis japonica in mice both prophylactically and therapeutocally, ninety-one compounds of substituted indanone and tetralone series were synthesized and twenty-three of them, all of which are in form of oximes, were effective in animal screening tests against Schistosoma japonicum.
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