1100361-45-2Relevant academic research and scientific papers
Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitors
Wu, Wen-Lian,Burnett, Duane A.,Clader, John,Greenlee, William J.,Jiang, Qin,Hyde, Lynn A.,Del Vecchio, Robert A.,Cohen-Williams, Mary E.,Song, Lixin,Lee, Julie,Terracina, Giuseppe,Zhang, Qi,Nomeir, Amin,Parker, Eric M.,Zhang, Lili
, p. 5836 - 5841 (2016/11/28)
In this paper we describe our strategy to improve the aqueous solubility of SCH 900229, a potent PS1-selective γ-secretase inhibitor for the treatment of Alzheimer's disease. Incorporation of ionizable amino groups into the side chain terminal generates w
Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors
Wu, Wen-Lian,Asberom, Theodros,Bara, Thomas,Bennett, Chad,Burnett, Duane A.,Clader, John,Domalski, Martin,Greenlee, William J.,Josien, Hubert,McBriar, Mark,Rajagopalan, Murali,Vicarel, Monica,Xu, Ruo,Hyde, Lynn A.,Del Vecchio, Robert A.,Cohen-Williams, Mary E.,Song, Lixin,Lee, Julie,Terracina, Giuseppe,Zhang, Qi,Nomeir, Amin,Parker, Eric M.,Zhang, Lili
, p. 844 - 849 (2013/02/25)
An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (-)-1a (SCH 900229), a potent, PS1-selective γ-secretase inhibitor and clinical candidate for the treatment of Alzheimer's disease. Specifically, 4-CF3 and 4-Br substituted arylsulfone analogs, (-)-1b and (-)-1c, are equipotent to compound (-)-1a. On the right hand side chain, linker size and terminal substituents of the pendant sulfone group are also investigated.
