几个含噻二唑环芳甲酰基脲的合成及生物活性
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O621.29

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湖北省自然科学基金(2008CDB016);湖北省教育厅青年项目(Q200729001)


Synthesis and Biological Activities of Several Aroyl Ureas Containing 1,3,4-Thiadiazole Unit
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    摘要:

    通过2-氨基-5-(3-吡啶基)-1,3,4-噻二唑与取代苯甲酰基异氰酸酯反应,得到相应的芳甲酰基脲IIIa~e,收率分别为69.5%、67.2%、73.1%、66.8%和71.6%。产物的结构经红外光谱、核磁共振氢谱、质谱与元素分析表征。并对目标化合物进行了植物生长调节活性测试,初步的测试结果表明,目标化合物在10 mg/L浓度下表现出一定程度的生长素活性和较好的细胞分裂素活性,其中N-[5-(3-吡啶基)-1,3,4-噻二唑-2-基]-N'-(4-溴苯甲酰基)脲(IIIc)和N-[5-(3-吡啶基)-1,3,4-噻二唑-2-基]-N'-(4-三氟甲基苯甲酰基)脲(IIIe)的细胞分裂素活性超过40%。

    Abstract:

    Several new aroyl ureas IIIa~e were synthesized by reaction of 2-amino-5-(3-pyridyl)-1,3,4-thiadiazole with substituted benzoyl isocyanates, in the yield of 69.5%, 67.2%, 73.1%, 66.8% and 71.6% respectively. The structures of the products were confirmed by IR, 1H NMR, MS and elemental analysis. The plant-growth regulating activities were tested on the title compounds. The results of preliminary tests indicated that these compounds exhibit some degree of auxin activity and relatively good cytokinin activity at the concentration of 10 mg/L, where the promoting rates towards cytokinin of N-(4-bromobenzoyl)-N'-[5-(3-pyridyl)-1,3,4-thiadiazol-2-yl]urea (IIIc) and N-[4-(trifluoromethyl)benzoyl]-N'-[5-(3-pyridyl)-1,3,4-thiadiazol-2-yl]urea (IIIe) reach above 40%.

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邵宇,杨平,宋新建,谭小红,余爱农.几个含噻二唑环芳甲酰基脲的合成及生物活性[J].精细化工,2010,27(7):

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  • 收稿日期:2010-02-20
  • 最后修改日期:2010-04-27
  • 录用日期:2010-04-28
  • 在线发布日期: 2010-06-25
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