Synthesis and Bioactivity of Novel N,N′-Diacylhydrazine Derivatives Containing Furan (II)
Synthesis and Bioactivity of Novel N,N′-Diacylhydrazine Derivatives Containing Furan (II)
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DOI：
10.1002/cjoc.201090214
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发表时间：
2010-07-01
影响因子：
5.4
通讯作者：
Ling Yun
中科院分区：
文献类型：
--
作者：
Li Xichen;Yang Xinling;Ling Yun
自1988年RH-5849被报道为第一个非甾体蜕皮激素激动剂以来，已发现二酰肼作为蜕皮激素类似物。近年来，含苯并含氧杂环的双酰基哌嗪类化合物的优化研究得到了广泛的关注。为了寻找具有高生物活性的新型化合物，设计合成了一系列含呋喃的单酰肼和双酰肼衍生物。它们的结构经H-1 NMR、IR、元素分析和单晶X-射线衍射分析证实。生物活性测定结果表明，部分单酰肼衍生物在10 mg/L时对淡色库蚊有较好的毒杀活性，且优于双酰肼衍生物。一般来说，双酰肼（II）的抗肿瘤活性优于单酰肼（I）。
Diacylhydrazines have been found as molting hormone analogs since RH-5849 was reported as the first nonsteroidal ecdysone agonist in 1988. Optimizations on diacylhydrizines with benzoheterocycle containing oxygen were widely explored in recent years. In order to find novel compounds with high bioactivity, a series of mono-(I) and di-acylhydrazine (II) derivatives containing furan were designed and synthesized. Their structures were confirmed by H-1 NMR, IR, elemental analyses and single crystal X-ray diffraction analyses (II7). The bioassay results showed that some of the mono-acylhydrazine (I) derivatives exhibited good larvicidal activity against Culex pipiens pallens at 10 mg/L and better than those of di-acylhydrazines (II). Generally, the anti-tumor activity of di-acylhydrazines (II) was better than that of mono-acylhydrazines (I).