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.
KeywordsMolecular hybridization Phthalimide Colitis Prednisolone Budesonide
The authors would like to thank the Brazilian Research Foundation FAPESP Process 2014/08728-6 for financial support.
Compliance with ethical standards
Conflict of interest
The authors declare that they have no conflict of interest.
The experiment and all the procedures were previously approved by the Research Ethics Committee of Animal Experimentation of the School of Pharmaceutical Sciences of Araraquara, São Paulo, Brazil (CEUA/FCFAr), under no. 11/2016. All procedures performed in studies involving animals were in accordance with the ethical standards of the institution or practice at which the studies were conducted.
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