| 曲智强,张玉镭,昝宁宁,姜 林.化学通报,2016,79(10):986-989. |
| 3-(3-吲哚基)-5-吡唑甲酰胺的合成及抑菌活性 |
| Synthesis and Antibacterial Activity of 3-(3-Indolyl)-5-pyrazole-5-carboxamide |
| 投稿时间：2016-01-09 修订日期：2016-03-15 |
| DOI： |
| 中文关键词: 吡唑 酰胺 吲哚 合成 抑菌活性 |
| 英文关键词:Pyrazole, Amide, Indole, Synthesis, Antifungal Activity |
| 基金项目:山东省科技发展计划(No. 2013GZX20109)资助项目 |
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| 中文摘要: |
| 本文以3-乙酰吲哚、草酸二乙酯、水合肼等为原料,经缩合、环化、水解反应制备3-(3-吲哚基)吡唑-5-甲酸,后者再与苄胺或2-苯乙胺在EDC-BTOH催化下合成了一系列N-取代苄基-3-(3-吲哚基)吡唑-5-甲酰胺和N-(2-取代苯基乙基)-3-(3-吲哚基)吡唑-5-甲酰胺。采用平板计数法测试了化合物对大肠杆菌和金黄色葡萄球菌的抑制活性,结果表明,在浓度为80 μg/mL时部分化合物有较高的抑菌活性。 |
| 英文摘要: |
| A series of novel N-substituted benzyl-3-(3-indolyl)pyrazole-3-carboxamides and N-(2-substituted phenyl ethyl)-3-(indol-3-yl)pyrazole-3-carboxamides were synthesized from 3-actyl indole, diethyl oxalate, hydrazine hydrate and benzylamine (or 2-phenylethylamine) by multi-step reactions. The target compounds were evaluated for their antifungal activities against E. coli and S. aureus, and the results indicated that some compounds displayed high antifungal activities at a concentration of 80μg/mL. |
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