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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.