Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369390 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
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.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Wen-Lian Wu, Theodros Asberom, Thomas Bara, Chad Bennett, Duane A. Burnett, John Clader, Martin Domalski, William J. Greenlee, Hubert Josien, Mark McBriar, Murali Rajagopalan, Monica Vicarel, Ruo Xu, Lynn A. Hyde, Robert A. Del Vecchio,