Publicação: Synthesis and anti-inflammatory intestinal activity of new glucocorticoid derivatives
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Glucocorticoids (GCs) are used worldwide in the treatment of chronic inflammatory diseases. This study describes the synthesis of new glucocorticoid derivatives and evaluates anti-inflammatory activity in rat models with ulcerative colitis (UC). Six compounds (5a–f) were synthetized using the molecular hybridization strategy with yields of 40–80%. The compounds 5e and 5f showed a total regression of ulceration in 83.3% and 75% of treated animals, respectively. Moreover, 5e improved several clinical signs, such as weight gain and survival rates. The compounds 5a and 5c showed total regression of ulceration in 33.3% of the rats. This is higher than prednisolone. Glucocorticoid derivatives showed potential anti-inflammatory intestinal activity with regression of ulceration in colitis.
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Budesonide, Colitis, Molecular hybridization, Phthalimide, Prednisolone
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Medicinal Chemistry Research, v. 29, n. 2, p. 206-216, 2020.
