State Key Laboratory of Elemento-Organic Chemistry, Nankai University, 94 Weijin Road, Nankai District, Tianjin 300071, People's Republic of China.
J Agric Food Chem. 2010 Jul 14;58(13):7846-55. doi: 10.1021/jf1006193.
1,2,3-Thiadiazoles, an important synthetic active substructure, are nowadays becoming one of the important branches in novel pesticide development. To develop pesticide candidates with diverse biological activities and probe their structure-activity relationship, three series of 5-methyl-1,2,3-thiadiazoles were rationally designed and synthesized using a simple and convenient one-step synthetic procedure via Ugi reaction. Biological activities of the target compounds including fungicidal activity, antivirus activity in vitro and in vivo, and systemic acquired resistance were systematically evaluated. The results indicated that compound III(10) showed broad-spectrum of activities against most fungi tested, and compounds I(10) and II(17) showed excellent potential antivirus activities as compared to positive control agent ribavirin. The preliminary structure-activity relationship was also discussed. The results of these studies indicated that the 5-position-substituted 1,2,3-thiadiazoles exhibited good antivirus activity and were worthy of further study in pesticide development.
1,2,3-噻二唑是一种重要的合成活性亚结构，如今已成为新型农药开发的重要分支之一。为了开发具有多样生物活性的农药候选物，并探究它们的构效关系，我们采用简便的 Ugi 反应一步合成法，合理设计并合成了三个系列的 5-甲基-1,2,3-噻二唑。我们系统地评估了目标化合物的杀菌活性、体外和体内抗病毒活性以及系统获得抗性。结果表明，化合物 III(10) 对大多数测试真菌表现出广谱活性，与阳性对照利巴韦林相比，化合物 I(10) 和 II(17) 表现出优异的潜在抗病毒活性。我们还讨论了初步的构效关系。这些研究结果表明，5-位取代的 1,2,3-噻二唑具有良好的抗病毒活性，值得进一步研究用于农药开发。
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