陆美贞, 唐佐君, 郑克勤, 章丽珠, 徐懋丽, 颜闵, 章元琅, 谢美华, 雷兴翰. 抗血吸虫病化合物:β-(5-硝基-2-呋喃)-丙烯酰二胺类衍生物的合成J. 药学学报, 1984, 19(7): 499-507.
引用本文: 陆美贞, 唐佐君, 郑克勤, 章丽珠, 徐懋丽, 颜闵, 章元琅, 谢美华, 雷兴翰. 抗血吸虫病化合物:β-(5-硝基-2-呋喃)-丙烯酰二胺类衍生物的合成J. 药学学报, 1984, 19(7): 499-507.
LU Mei-Zhen, TANG Zuo-Jun, ZHENG Ke-Qin, ZHANG Li-Zhu, XU Mao-Li, YAN Min, ZHANG Yuan-Lang, XIE Mei-Hua , LEI Xing-Han, . SYNTHESIS OF SCHISTOSOMICIDAL COMPOUNDS: DIALKYLAMINOALKYLAMINO DERIVATIVES OF β-(5-NITRO-2-FURYL)-ACRYLAMIDEJ. Acta Pharmaceutica Sinica, 1984, 19(7): 499-507.
Citation: LU Mei-Zhen, TANG Zuo-Jun, ZHENG Ke-Qin, ZHANG Li-Zhu, XU Mao-Li, YAN Min, ZHANG Yuan-Lang, XIE Mei-Hua , LEI Xing-Han, . SYNTHESIS OF SCHISTOSOMICIDAL COMPOUNDS: DIALKYLAMINOALKYLAMINO DERIVATIVES OF β-(5-NITRO-2-FURYL)-ACRYLAMIDEJ. Acta Pharmaceutica Sinica, 1984, 19(7): 499-507.

抗血吸虫病化合物:β-(5-硝基-2-呋喃)-丙烯酰二胺类衍生物的合成

SYNTHESIS OF SCHISTOSOMICIDAL COMPOUNDS: DIALKYLAMINOALKYLAMINO DERIVATIVES OF β-(5-NITRO-2-FURYL)-ACRYLAMIDE

  • 摘要: 本文报道70个β-(5-硝基-2-呋喃)-丙烯酰二胺类衍生物的合成。对感染日本血吸虫病小白鼠进行治疗和预防初筛的结果,发现有54个化合物具有不同程度的抗虫作用。其中以反式β-(5-硝基2-呋喃)-N-(2-哌啶乙基)丙烯酰胺盐酸盐(I13,F-30385)及其盐基呋喃双胺(I14,F-30642)杀虫作用最强,均已试用于临床,后者疗效较好,副作用较轻。

     

    Abstract: In order to prove the possibility of increasing the schistosomicidal activity, a basic side chain was introduced to nitrofurylacrylamide. The key intermediates of various dialkylaminoalkylamines were prepared by known methods and condensed with β-(5-nitro-2-furyl)-acryloyl chloride to form the corresponding basic amides.In screening with mice infected with Schistosoma japonicum, fifty four out of seventy compounds were found to possess pronounced antischistosomal action. Among these, N-(2-piperidinoethylamino)-β-(5-nitro-2-furyl)acrylamide hydrochloride I13 (F-30385) and its base I14 (F-30642) were shown to be the most effective and tested clinically. The latter compound was shown to have lower adverse reaction with higher therapeutic efficacy than Furapromidium.

     

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