Design, synthesis, and pharmacological effects of a cyclization-activated steroid prodrug for colon targeting in inflammatory bowel disease

JFM Ruiz, G Radics, H Windle, HO Serra…

Index: Marquez Ruiz, Juan F.; Radics, Gabor; Windle, Henry; Serra, Hugo O.; Simplicio, Ana Luisa; Kedziora, Kinga; Fallon, Padraic G.; Kelleher, Dermot P.; Gilmer, John F. Journal of Medicinal Chemistry, 2009 , vol. 52, # 10 p. 3205 - 3211

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Citation Number: 23

Abstract

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 ...