| 血吸虫病化学治疗的研究——ⅩⅪⅤ.5-[2-(5-硝基呋喃基-2)-1-取代乙烯基]-1,3,4-噁二唑酮及其1,3,4-噁二唑衍生物的合成 |
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| 引用本文： | 陈文彬,王保钧,陈宝珍,章丽珠,颜闵,雷兴翰.血吸虫病化学治疗的研究——ⅩⅪⅤ.5-[2-(5-硝基呋喃基-2)-1-取代乙烯基]-1,3,4-噁二唑酮及其1,3,4-噁二唑衍生物的合成[J].药学学报,1986,21(10):761-766. |
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| 作者姓名： | 陈文彬 王保钧 陈宝珍 章丽珠 颜闵 雷兴翰 |
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| 作者单位： | 上海医药工业研究院 |
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| 摘 要： | 本文报道硝基呋喃乙烯基-1,3,4-噁二唑及其酮类衍生物44个的合成。关键中间体α-取代β-(5-硝基呋喃基-2)丙烯酰彤魄仿照文献已知方法制备的,然后分别与光气或溴化腈作用生成相应的1,3,4-噁二唑衍生物Ⅰ,Ⅱ。经感染日本血吸虫病小白鼠的预防和治疗试验,发现化合物Ⅰ1具有显著的抗血吸虫作用,并试用于家犬的血吸虫病,证明有一定的疗效。但效果不及呋喃丙胺,故未作临床观察。
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| 关 键 词： | 抗日本血吸虫作用 硝基呋喃乙烯基-1 3 4-(口恶)二唑衍生物 |
| 收稿时间： | 1985-12-04 |
Chemotherapeutic studies on schistosomiasis. XXIV. Synthesis of derivatives of 5-[2-(5-nitro-furyl-2)-1-substituted vinyl]-1,3,4-oxadiazol-2-one and its 1,3,4-oxadiazol |
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| CHEN Wen-Bin,WANG Bao-Jun,CHEN Bao-Zhen,ZHANG Li-Zhu,YAN Min and LEI Xing-Han.Chemotherapeutic studies on schistosomiasis. XXIV. Synthesis of derivatives of 5-[2-(5-nitro-furyl-2)-1-substituted vinyl]-1,3,4-oxadiazol-2-one and its 1,3,4-oxadiazol[J].Acta Pharmaceutica Sinica,1986,21(10):761-766. |
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| Authors: | CHEN Wen-Bin WANG Bao-Jun CHEN Bao-Zhen ZHANG Li-Zhu YAN Min and LEI Xing-Han |
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| Abstract: | Forty-four compounds of nitrofuranvinyl-1,3,4-oxadiazol-2-one and its 1,3,4-oxadiazole have been synthesized. The key intermediate, α-substituted 5-nitro-2-furylacryloylhydrazine, was prepared by known method and it reacted subsequently with phosgen or bromocyanogen to form the corresponding 1,3,4-oxadiazolone of compound Ⅰ and Ⅱ respectively. |
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| Keywords: | 5-[2-(5-nitro furyl-2)-1-substituted vinyl]-1 3 4-oxadiazol-2-one Schistosonia Japonicum |
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