Pyridine-derived γ-secretase modulators
Copyright policy )Pyridine-derived γ-secretase modulators
SAR of a novel series of pyridine-derived γ-secretase modulators is described. Compound 5 was found to be a potent modulator in vitro, which on further profiling, was found to decrease Aβ42 and Aβ40, and maintain (or increase) the levels of total Aβ. Furthermore, representative compounds 1 and 5 demonstrated in vivo efficacy to lower Aβ42 in the brain without altering Notch processing in the peripheral.
- Cellzome, GSK, Middlesex, UK.
- GlaxoSmithKline (China) China (People's Republic of)
Dose-Response Relationship, Drug, Molecular Structure, Pyridines, Biological Availability, Stereoisomerism, Rats, Structure-Activity Relationship, Animals, Cytochrome P-450 Enzyme Inhibitors, Humans, Amyloid Precursor Protein Secretases, Enzyme Inhibitors
Dose-Response Relationship, Drug, Molecular Structure, Pyridines, Biological Availability, Stereoisomerism, Rats, Structure-Activity Relationship, Animals, Cytochrome P-450 Enzyme Inhibitors, Humans, Amyloid Precursor Protein Secretases, Enzyme Inhibitors
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