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ID: ALA1155995

Journal: Bioorg Med Chem Lett

Title: Pyrrole[2,3-d]azepino compounds as agonists of the farnesoid X receptor (FXR).

Authors: Mehlmann JF, Crawley ML, Lundquist JT, Unwalla RJ, Harnish DC, Evans MJ, Kim CY, Wrobel JE, Mahaney PE.

Abstract: Pyrrole[2,3-d]azepines have been identified as potent agonists of the farnesoid X receptor (FXR). Based on the planar X-ray crystal structure of WAY-362450 1 in the ligand binding domain and molecular modeling studies, non-planar reduced compounds were designed which led to agonists that exhibit high aqueous solubility and retain moderate in vitro potency.

CiteXplore: 19683924

DOI: 10.1016/j.bmcl.2009.07.148