Piperidine-derived gamma-secretase modulators.

Hall, A., Elliott, R.L., Giblin, G.M., Hussain, I., Musgrave, J., Naylor, A., Sasse, R., Smith, B.
Journal   Bioorg Med Chem Lett
Species  
Analytes Measured   Abeta 40 , Abeta 42
Matrix Tested   SHSY5Y neuroblast cell lysates
Year   2010
Volume   20
Page Numbers   1306-11
Application   Alzheimers
Abstract
This Letter details the SAR of a novel series of piperidine-derived gamma-secretase modulators. Compound 10h was found to be a potent modulator in vitro, which on further profiling, was found to decrease Abeta42, increase Abeta38 and have no effect on Abeta40 levels. Furthermore, 10h demonstrated excellent pharmacokinetic parameters in the mouse, rat and dog in addition to good CNS penetration in the mouse.

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