抗血吸虫病药物呋喃丙胺顺式异构体的研究
THE CIS-ISOMER OF ANTISHISTOSOMAL DRUG FURAPROMIDE
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摘要: 呋喃丙胺顺式异构体的合成,系按文献方法制备顺式β-(5-硝基-2-呋喃)-丙烯酸,然后于低温下与异丙胺经混合酸酐法,氨化为顺式与反式两种酰胺的混合物,再经分离获得顺式异构体。实验动物药理结果证明其生物活性与反式异构体相似。Abstract: Nitration of cis-β-(2-furyl) acrylic acid afforded the corresponding cis-β-(5-nitro-furyl), acrylic acid. It was readily converted to cis-β-(5-nitro-2-furyl)-N-isopropyl-acrylamide by amination with isopropylamine through the mixed anhydride method.The biological activity of this cis-isomer was examined in laboratory animals against experimental schistosomiasis and was shown to possess activity similar to that already reported for the trans-isomer.
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