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Synthesis and Anti-Inflammatory Activity of New Alkyl-Substituted Phthalimide 1H-123-Triazole Derivatives

机译:新型烷基取代的邻苯二甲酰亚胺1H-123-三唑衍生物的合成及抗炎活性

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摘要

Four new 1,2,3-triazole phthalimide derivatives with a potent anti-inflammatory activity have been synthesized in the good yields by the 1,3-dipolar cycloaddition reaction from N-(azido-alkyl)phthalimides and terminal alkynes. The anti-inflammatory activity was determined by injecting carrageenan through the plantar tissue of the right hind paw of Swiss white mice to produce inflammation. All the compounds >3a–c and >5a–c exhibited an important anti-inflammatory activity; the best activity was found for the compounds >3b and >5c, which showed to be able to decrease by 69% and 56.2% carrageenan-induced edema in mice. These compounds may also offer a future promise as a new anti-inflammatory agent.
机译:N-(叠氮基-烷基)邻苯二甲酰亚胺和末端炔烃通过1,3-偶极环加成反应以高收率合成了四种具有有效抗炎活性的新的1,2,3-三唑邻苯二甲酰亚胺衍生物。通过将角叉菜胶通过瑞士白小鼠右后爪的足底组织注射以产生炎症来确定抗炎活性。所有化合物> 3a–c 和> 5a–c 均显示出重要的抗炎活性。化合物> 3b 和> 5c 的活性最佳,表明能够减少角叉菜胶引起的小鼠水肿的69%和56.2%。这些化合物也有望作为一种新型的抗炎药。

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