Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent γ-secretase inhibitors
…, J Wells, BM Cochran, MA Wolf, LA Thompson…
文献索引：Yang, Michael G.; Shi, Jian-Liang; Modi, Dilip P.; Wells, Jennifer; Cochran, Brian M.; Wolf, Mark A.; Thompson, Lorin A.; Ramanjulu, Mercy M.; Roach, Arthur H.; Zaczek, Robert; Robertson, David W.; Wexler, Ruth R.; Olson, Richard E. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 14 p. 3910 - 3915
We report the synthesis of benzoazepine-derived cyclic malonamides (2) and aminoamides (3) as γ-secretase inhibitors for the potential treatment of Alzheimer's disease. The in vitro structure–activity relationships of 2 and 3 along with dog pharmacokinetic results are described.
