Author(s): Machado, Marcella Gabrielle Mendes [UNESP] ; Scarim, Cauê Benito [UNESP] ; de Andrade, Cleverton Roberto [UNESP] ; dos Santos, Jean Leandro [UNESP] ; Chin, Chung Man [UNESP]
Date: 2020
Persistent ID: http://hdl.handle.net/11449/201339
Origin: Oasisbr
Subject(s): Budesonide; Colitis; Molecular hybridization; Phthalimide; Prednisolone; Budesonide; Budesonide; Colitis; Colitis; Molecular hybridization; Molecular hybridization; Phthalimide; Phthalimide; Prednisolone; Prednisolone
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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.
School of Pharmaceutical Sciences São Paulo State University (UNESP), Rodovia Araraquara-Jaú km-1 s/n, campus ville
School of Dentistry São Paulo State University (UNESP)
School of Pharmaceutical Sciences São Paulo State University (UNESP), Rodovia Araraquara-Jaú km-1 s/n, campus ville
School of Dentistry São Paulo State University (UNESP)
