Design, Synthesis and Bioactivity of Novel Glycosylthiadiazole Derivatives

文献类型: 外文期刊

第一作者: Zong, Guanghui

作者: Zong, Guanghui;Zhao, Hanqing;Jiang, Rui;Zhang, Jianjun;Liang, Xiaomei;Wang, Daoquan;Zhao, Hanqing;Li, Baoju;Shi, Yanxia

作者机构:

关键词: 1;3;4-thiadiazole;carbohydrates;synthesis;fungicidal activity

期刊名称:MOLECULES ( 影响因子:4.411; 五年影响因子:4.587 )

ISSN:

年卷期:

页码:

收录情况: SCI

摘要: A series of novel glycosylthiadiazole derivatives, namely 2-phenylamino-5- glycosyl-1,3,4-thiadiazoles, were designed and synthesized by condensation between sugar aldehydes A/B and substituted thiosemicarbazide C followed by oxidative cyclization by treating with manganese dioxide. The original fungicidal activities results showed that some title compounds exhibited excellent fungicidal activities against Sclerotinia sclerotiorum (Lib.) de Bary and Pyricularia oryzae Cav, especially compounds F-5 and G-8 which displayed better fungicidal activities than the commercial fungicide chlorothalonil. At the same time, the preliminary studies based on the Elson-Morgan method indicated that many compounds exhibited some inhibitory activity toward glucosamine-6- phosphate synthase (GlmS). The structure-activity relationships (SAR) are discussed in terms of the effects of the substituents on both the benzene and the sugar ring.

分类号: O62

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