Purine derivatives as potent g-secretase modulators

The development of a novel series of purines as g-secretase modulators for potential use in the treatment of Alzheimer's disease is disclosed herein. Optimization of a previously disclosed pyrimidine series afforded a series of potent purine-based g-secretase modulators with 300- to 2000-fold i...

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Published inBioorganic & medicinal chemistry letters Vol. 20; no. 7; pp. 2279 - 2282
Main Authors Rivkin, Alexey, Ahearn, Sean P, Chichetti, Stephanie M, Hamblett, Christopher L, Garcia, Yudith, Martinez, Michelle, Hubbs, Jed L, Reutershan, Michael H, Daniels, Matthew H, Siliphaivanh, Phieng, Otte, Karin M, Li, Chaomin, Rosenau, Andrew, Surdi, Laura M, Jung, Joon, Hughes, Bethany L, Crispino, Jamie L, Nikov, George N, Middleton, Richard E, Moxham, Christopher M, Szewczak, Alexander A, Shah, Sanjiv, Moy, Lily Y, Kenific, Candia M, Tanga, Flobert, Cruz, Jonathan C, Andrade, Paula, Angagaw, Minilik H, Shomer, Nirah H, Miller, Thomas, Munoz, Benito, Shearman, Mark S
Format Journal Article
LanguageEnglish
Published 01.04.2010
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Summary:The development of a novel series of purines as g-secretase modulators for potential use in the treatment of Alzheimer's disease is disclosed herein. Optimization of a previously disclosed pyrimidine series afforded a series of potent purine-based g-secretase modulators with 300- to 2000-fold in vitro selectivity over inhibition of Notch cleavage and that selectively reduces Ab42 in an APP-YAC transgenic mouse model. AB:
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.02.008