pf-3084014 and tetralin

pf-3084014 has been researched along with tetralin* in 1 studies

Other Studies

1 other study(ies) available for pf-3084014 and tetralin

Article	Year
Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014. Bioorganic & medicinal chemistry letters, 2011, May-01, Volume: 21, Issue:9 A novel series of tetralin containing amino imidazoles, derived from modification of the corresponding phenyl acetic acid derivatives is described. Replacement of the amide led to identification of a potent series of tetralin-amino imidazoles with robust central efficacy. The reduction of brain Aβ in guinea pigs in the absence of changes in B-cells suggested a potential therapeutic index with respect to APP processing compared with biomarkers of notch related toxicity. Optimization of the FTOC to plasma concentrations at the brain Aβ EC(50) lead to the identification of compound 14f (PF-3084014) which was selected for clinical development. Topics: Amyloid Precursor Protein Secretases; Animals; Biological Assay; Drug Design; Enzyme Activation; Enzyme Inhibitors; Guinea Pigs; Imidazoles; Inhibitory Concentration 50; Molecular Structure; Structure-Activity Relationship; Tetrahydronaphthalenes; Valine	2011

Article

Year

Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014.

Bioorganic & medicinal chemistry letters, 2011, May-01, Volume: 21, Issue:9

A novel series of tetralin containing amino imidazoles, derived from modification of the corresponding phenyl acetic acid derivatives is described. Replacement of the amide led to identification of a potent series of tetralin-amino imidazoles with robust central efficacy. The reduction of brain Aβ in guinea pigs in the absence of changes in B-cells suggested a potential therapeutic index with respect to APP processing compared with biomarkers of notch related toxicity. Optimization of the FTOC to plasma concentrations at the brain Aβ EC(50) lead to the identification of compound 14f (PF-3084014) which was selected for clinical development.

Topics: Amyloid Precursor Protein Secretases; Animals; Biological Assay; Drug Design; Enzyme Activation; Enzyme Inhibitors; Guinea Pigs; Imidazoles; Inhibitory Concentration 50; Molecular Structure; Structure-Activity Relationship; Tetrahydronaphthalenes; Valine

2011