【摘要】 <正> 著名抗曼氏血吸虫病药羟蒽酮(Hycanthone)(Ⅱ_b)是硫蒽酮(Lucanthone)(Ⅱ_a)分子上甲基转化为羟甲基的衍生物。Rosi等发现麴霉菌能将硫蒽酮生化转化生成羟蒽酮。经物理、化学和生物试验,证明它是硫蒽酮的代谢产物。动物实验结果表明,羟蒽酮抗小白鼠及田鼠曼氏血吸虫病的作用比硫蒽酮分别大3及9倍。此种效应也出现在2-异丙氨甲基-6-甲更多还原

【Abstract】 In view of the fact that the schistosomicidal activity of lucanthone and UK 3883 has been markedly enhanced by methanolization, niridazolylmethanol and its esters were synthesized through esterification of niridazolylmethanol with acyl chlorides or anhydrides of appropriate acids. Most of the esters were shown to possess pronounced antischistosomal activity in mice infected with Schistosomasis japonica. The structureactivity relationship was discussed.更多还原