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| 新型N-(5-烷基-1,3,4-噻二唑-2-基)-1-[(杂芳基)甲基]-5-甲基-1H-1,2,3-三唑基-4-甲酰胺的合成与生物活性 | |
| 引用本文： | 陈小保,石德清. 新型N-(5-烷基-1,3,4-噻二唑-2-基)-1-[(杂芳基)甲基]-5-甲基-1H-1,2,3-三唑基-4-甲酰胺的合成与生物活性[J]. 有机化学, 2009, 29(7): 1100-1104 |
| 作者姓名： | 陈小保 石德清 |
| 作者单位： | (a华中师范大学化学学院 农药与化学生物学教育部重点实验室 武汉 430079) ;(b郧阳医学院药物化学系 十堰 442000) ; |
| 摘 要： | 为了寻找新型高效低毒的农药先导化合物, 采用1-[(杂芳基)甲基]-5-甲基-1H-1,2,3-三唑基-4-甲酰氯与2-氨基-5-烷基-1,3,4-噻二唑的缩合反应, 合成了8种未见文献报道的目标化合物, 其结构经IR, 1H NMR和元素分析确证, 部分化合物还经MS的进一步证实. 初步的生物活性测试结果表明, 部分目标化合物在100 mg/L浓度下对双子叶植物(油菜)显示出中等的除草活性和一定程度的杀虫活性(250 mg/L). |
| 关 键 词： | 取代吡啶 噻唑 1,2,3-三唑 1,3,4-噻二唑 生物活性 |
| 收稿时间： | 2008-12-02 |
| 修稿时间： | 2008-12-22 |
Synthesis and Biological Activities of Novel N-(5-Alkyl-1,3,4- thiadiazol-2-yl)-1-[(heteroaryl)methyl]-5-methyl-1H-1,2,3- triazole-4-carboxamides |
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| Affiliation: | (a Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079) (b Department of Medicinal Chemistry, Yunyang Medical College, Shiyan 442000) |
| Abstract: | In search of novel low toxicity and potent pesticide lead compounds, eight title compounds were synthesized via the condensation reactions of 1-[(heteroaryl)methyl]-5-methyl-1H-1,2,3-triazole-4-carbonyl chlorides with 5-alkyl-2-amino-1,3,4-thiadiazoles, and structurally characterized by IR, 1H NMR spectra, and elemental analysis or further by MS technique. Preliminary bioassays showed that a fraction of the target compounds possessed moderate herbicidal activities against dicotyledonous plants (Brassica campestris L) at the concerntration of 100 mg/L and insecticidal activity to some extent at the concerntration of 250 mg/L. |
| Keywords: | substituted pyridine thiazole 1,2,3-triazole 1,3,4-thiadiazole biological activity |
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