107921-07-3Relevant academic research and scientific papers
Design and Synthesis of N-Arylphthalimides as Inhibitors of Glucocorticoid-Induced TNF Receptor-Related Protein, Proinflammatory Mediators, and Cytokines in Carrageenan-Induced Lung Inflammation
Bhat, Mashooq A.,Al-Omar, Mohamed A.,Ansari, Mushtaq A.,Zoheir, Khairy M. A.,Imam, Faisal,Attia, Sabry M.,Bakheet, Saleh A.,Nadeem, Ahmed,Korashy, Hesham M.,Voronkov, Andrey,Berishvili, Vladimir,Ahmad, Sheikh F.
, p. 8850 - 8867 (2015)
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.
Mechanistic differences between in vitro assays for hydrazone-based small molecule inhibitors of anthrax lethal factor
Hanna, M. Leslie,Tarasow, Theodore M.,Perkins, Julie
, p. 50 - 58 (2008/09/18)
A systematically generated series of hydrazones were analyzed as potential inhibitors of anthrax lethal factor. The hydrazones were screened using one UV-based and two fluorescence-based in vitro assays. The study identified several inhibitors with IC50 values in the micromolar range, and importantly, significant differences in the types of inhibition were observed with the different assays.
