258870-47-2Relevant academic research and scientific papers
Synthesis and evaluation of succinoyl-caprolactam γ-secretase inhibitors
Thompson, Lorin A.,Liauw, Ann Y.,Ramanjulu, Mercy M.,Kasireddy-Polam, Padmaja,Mercer, Stephen E.,Maduskuie, Thomas P.,Glicksman, Marcie,Roach, Arthur H.,Meredith, Jere E.,Liu, Rui-Qin,Combs, Andrew P.,Higaki, Jeffrey N.,Cordell, Barbara,Seiffert, Dietmar,Zaczek, Robert C.,Robertson, David W.,Olson, Richard E.
, p. 2357 - 2363 (2006)
The synthesis, evaluation, and structure-activity relationships of a series of succinoyl lactam inhibitors of the Alzheimer's disease γ-secretase are described. Beginning with a screening hit with broad proteinase activity, optimization provided compounds with both high selectivity for inhibition of γ-secretase and high potency in cellular assays of Aβ reduction. The SAR and early in vivo properties of this series of inhibitors will be presented.
