2666-20-8Relevant academic research and scientific papers
Design, synthesis, and pharmacological effects of a cyclization-activated steroid prodrug for colon targeting in inflammatory bowel disease
Márquez Ruiz, Juan F.,Radics, Gabor,Windle, Henry,Serra, Hugo O.,Simplício, Ana Luísa,Kedziora, Kinga,Fallon, Padraic G.,Kelleher, Dermot P.,Gilmer, John F.
supporting information; experimental part, p. 3205 - 3211 (2010/03/24)
Glucocorticoids are used in the treatment of inflammatory bowel disease. A limitation to their use is that they undergo absorption from the GIT before reaching the colon causing severe systemic side effects. We report here on a novel prodrug approach to targeting corticosteroids to the colon. The design involves attaching a 21-ester group that suppresses absorption during transit to the colon. The prodrug is designed to be primed by colonic microflora liberating an amino ester that cyclizes releasing the steroid. One of the prodrugs 5b was as efficacious as prednisolone in the murine DSS model but did not cause thymic atrophy, a marker for systemic steroid effects.
Synthesis and pregnancy terminating activity of pyrazolo[1,5-a]indoles and quinolines
Winters,Odasso,Conti,et al.
, p. 215 - 218 (2007/10/02)
In order to clarify the structural requirements for antifertility activity, series of 2-arylpyrazolo[1,5-a]indoles and 2-arylpyrazolo[1,5-a]-quinolines were prepared and tested in rats and hamsters. Their potencies were compared with those of the isomeric
