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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Synthesis and anti-inflammatory intestinal activity of new glucocorticoid derivatives

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Author(s):
Mendes Machado, Marcella Gabrielle [1] ; Scarim, Caue Benito [1] ; de Andrade, Cleverton Roberto [2] ; dos Santos, Jean Leandro [1] ; Chin, Chung Man [1]
Total Authors: 5
Affiliation:
[1] Sao Paulo State Univ UNESP, Sch Pharmaceut Sci, BR-14800903 Araraquara, SP - Brazil
[2] Sao Paulo State Univ Unesp, Sch Dent, Araraquara, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Source: MEDICINAL CHEMISTRY RESEARCH; v. 29, n. 2 NOV 2019.
Web of Science Citations: 0
Abstract

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. (AU)

FAPESP's process: 14/08728-6 - Design and synthesis of new anti-inflammatory steroids of Lapdesf FT-GL and GL-TAU series with potential anti-VEGF activity
Grantee:Marcella Gabrielle Mendes Machado
Support Opportunities: Scholarships in Brazil - Doctorate