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ID: ALA4265914

Journal: Bioorg Med Chem Lett

Title: Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.

Authors: Islam I, Yuan S, West CW, Adler M, Bothe U, Bryant J, Chang Z, Chu K, Emayan K, Gualtieri G, Ho E, Light D, Mallari C, Morser J, Phillips G, Schaefer C, Sukovich D, Whitlow M, Chen D, Buckman BO.

Abstract: We report here the design and synthesis of a novel series of benzylamines that are potent and selective inhibitors of uPA with promising oral availability in rat. Further evaluation of one representative (ZK824859) of the new structural class showed that this compound lowered clinical scores when dosed in either acute or chronic mouse EAE models, suggesting that uPA inhibitors of this type could be useful for the treatment of multiple sclerosis.

CiteXplore: 30201291

DOI: 10.1016/j.bmcl.2018.09.001