930100-79-1Relevant academic research and scientific papers
Diamide amino-imidazoles: A novel series of γ-secretase inhibitors for the treatment of Alzheimers disease
Brodney, Michael A.,Auperin, David D.,Becker, Stacey L.,Bronk, Brian S.,Brown, Tracy M.,Coffman, Karen J.,Finley, James E.,Hicks, Carol D.,Karmilowicz, Michael J.,Lanz, Thomas A.,Liston, Dane,Liu, Xingrong,Martin, Barbara-Anne,Nelson, Robert B.,Nolan, Charles E.,Oborski, Christine E.,Parker, Christine P.,Richter, Karl E.G.,Pozdnyakov, Nikolay,Sahagan, Barbara G.,Schachter, Joel B.,Sokolowski, Sharon A.,Tate, Barbara,Van Deusen, Jeffrey W.,Wood, Douglas E.,Wood, Kathleen M.
, p. 2631 - 2636 (2011/06/20)
The synthesis and structure-activity relationship (SAR) of a novel series of di-substituted imidazoles, derived from modification of DAPT, are described. Subsequent optimization led to identification of a highly potent series of inhibitors that contain a β-amine in the imidazole side-chain resulting in a robust in vivo reduction of plasma and brain Aβ in guinea pigs. The therapeutic index between Aβ reductions and changes in B-cell populations were studied for compound 10h.
