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新型烷基取代邻苯二甲酰亚胺1H-1,2,3-三唑衍生物的合成与抗炎活性

Synthesis and anti-inflammatory activity of new alkyl-substituted phthalimide 1H-1,2,3-triazole derivatives.

作者信息

Assis Shalom Pôrto de Oliveira, da Silva Moara Targino, de Oliveira Ronaldo Nascimento, Lima Vera Lúcia de Menezes

机构信息

Laboratório de Química e Metabolismo de Lipídeos e Lipoproteínas, Departamento de Bioquímica, Universidade Federal de Pernambuco (UFPE), Avenida Prof. Moraes Rego s/n, 50670-420 Recife, PE, Brazil.

出版信息

ScientificWorldJournal. 2012;2012:925925. doi: 10.1100/2012/925925. Epub 2012 Dec 5.

Abstract

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.

摘要

通过N-(叠氮基烷基)邻苯二甲酰亚胺与末端炔烃的1,3-偶极环加成反应,以良好的产率合成了四种具有强效抗炎活性的新型1,2,3-三唑邻苯二甲酰亚胺衍生物。通过向瑞士小白鼠右后爪的足底组织注射角叉菜胶以引发炎症来测定抗炎活性。所有化合物3a-c和5a-c均表现出重要的抗炎活性;化合物3b和5c的活性最佳,它们能够使小鼠角叉菜胶诱导的水肿分别减少69%和56.2%。这些化合物作为一种新型抗炎剂也可能具有未来前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c5e/3523591/0333c891fa27/TSWJ2012-925925.001.jpg

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