Marquez Ruiz, Juan F.; Kedziora, Kinga; O’Reilly, Mary; Maguire, Jacqueline; Keogh, Brian; Windle, Henry; Kelleher, Dermot P.; Gilmer, John F. published the artcile< Azo-reductase activated budesonide prodrugs for colon targeting>, SDS of cas: 30095-98-8, the main research area is azoreductase budesonide prodrug colon targeting.
Budesonide is a synthetic glurocorticoid that undergoes substantial first pass metabolism, limiting systemic exposure. Its use in treatment of inflammatory bowel disease would benefit from a targeting strategy that could lead to a local topical effect, improving safety and increasing anti-inflammatory efficacy. A two-step prodrug strategy involving azoredn./cyclization that we developed previously for prednisolone is here applied with some variations to budesonide. The budesonide prodrugs were tested using an in vitro azoreductase assay simulating human colonic microflora. The kinetics of amino steroid ester cyclization and its pH dependence was also evaluated. The stability of the prodrugs systems in simulated human duodenal and gastric fluid was evaluated to determine the likelihood of intact intestinal transit. The propionic acid derived prodrug 3 undergoes rapid activation by Clostridium perfingens and its putative reduction product cyclizes with acceptable rapidity when synthesized independently. These properties of 3 suggest that it has potential in management of ulcerative colitis.
Bioorganic & Medicinal Chemistry Letters published new progress about Anti-inflammatory agents. 30095-98-8 belongs to class esters-buliding-blocks, and the molecular formula is C9H9NO4, SDS of cas: 30095-98-8.
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