921599-79-3Relevant academic research and scientific papers
Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency
Egbertson, Melissa,McGaughey, Georgia B.,Pitzenberger, Steven M.,Stauffer, Shaun R.,Coburn, Craig A.,Stachel, Shawn J.,Yang, Wenjin,Barrow, James C.,Neilson, Lou Anne,McWherter, Melody,Perlow, Debra,Fahr, Bruce,Munshi, Sanjeev,Allison, Timothy J.,Holloway, Katharine,Selnick, Harold G.,Yang, Zhiqiang,Swestock, John,Simon, Adam J.,Sankaranarayanan, Sethu,Colussi, Dennis,Tugusheva, Katherine,Lai, Ming-Tain,Pietrak, Beth,Haugabook, Shari,Jin, Lixia,Chen,Holahan, Marie,Stranieri-Michener, Maria,Cook, Jacquelynn J.,Vacca, Joseph,Graham, Samuel L.
, p. 4812 - 4819 (2015/10/28)
The IC50 of a beta-secretase (BACE-1) lead compound was improved ～200-fold from 11 μM to 55 nM through the addition of a single methyl group. Computational chemistry, small molecule NMR, and protein crystallography capabilities were used to com
SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 41, (2010/11/25)
The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as
