Design and Synthesis of N-Arylphthalimides as Inhibitors of Glucocorticoid-Induced TNF Receptor-Related Protein, Proinflammatory Mediators, and Cytokines in Carrageenan-Induced Lung Inflammationстатья

Статья опубликована в высокорейтинговом журнале

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Дата последнего поиска статьи во внешних источниках: 23 ноября 2017 г.

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[1] Design and synthesis of n-arylphthalimides as inhibitors of glucocorticoid-induced tnf receptor-related protein, proinflammatory mediators, and cytokines in carrageenan-induced lung inflammation / M. Bhat, M. Al-Omar, M. Ansari et al. // Journal of Medicinal Chemistry. — 2015. — Vol. 58, no. 22. — P. 8850–8867. N-Arylphthalimides (1–10P) derived from thalidomide by insertion of hydrophobic groups were evaluated for anti-inflammatory activity, and (4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N′-[(4-ethoxyphenyl)methylidene]benzohydrazide 6P was identified as a promising anti-inflammatory agent. Further testing confirmed that compared with the control, 6P treatment resulted in a considerable decrease in CD4+, NF-κB p65+, TNF-α+, IL-6+, GITR+, and IL-17+ cell populations and an increase in the Foxp3+, CD4+Foxp3+, and IκBα+ populations in whole blood and pleural fluid of a mouse model of lung inflammation. Moreover, treatment with compound 6P decreased the proteins associated with inflammation including TNF-α, IL-6, IL-17, GITR, NF-κB, COX-2, STAT-3, and iNOS and increased the anti-inflammatory mediators such as IL-10 and IL-4. Further, histopathological examination confirmed the potent anti-inflammatory effects of compound 6P. Thus, the N-arylphthalimide derivative 6P acts as a potent anti-inflammatory agent in the carrageenan-induced lung inflammation model, suggesting that this compound may be useful for the treatment of inflammation in a clinical setting. [ DOI ]

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