Compounds > 4-(6-iodo-2-imidazo[1-2-a]pyridinyl)-N-N-dimethylaniline

4-(6-iodo-2-imidazo[1-2-a]pyridinyl)-N-N-dimethylaniline and dibenzylidene-acetone

4-(6-iodo-2-imidazo[1-2-a]pyridinyl)-N-N-dimethylaniline has been researched along with dibenzylidene-acetone* in 1 studies

Other Studies

1 other study(ies) available for 4-(6-iodo-2-imidazo[1-2-a]pyridinyl)-N-N-dimethylaniline and dibenzylidene-acetone

Article	Year
Synthesis and structure-affinity relationships of novel dibenzylideneacetone derivatives as probes for β-amyloid plaques. Journal of medicinal chemistry, 2011, Apr-14, Volume: 54, Issue:7 A new and extensive set of dibenzylideneacetone derivatives was synthesized and screened for affinity toward Aβ(1-42) aggregates. Structure-activity relationships revealed the binding of dibenzylideneacetones to be affected by various substituents. The introduction of a substituent group in the ortho position reduced or abolished the binding. However, the para position was highly tolerant of sterically demanding substitutions. Three radioiodinated ligands (6, 70, and 71) and two (18)F fluoro-pegylated (FPEG) ligands (83 and 85) were prepared, all of which displayed high affinity for Aβ(1-42) aggregates (K(i) ranging from 0.9 to 7.0 nM). In biodistribution experiments, they exhibited good initial penetration (1.59, 4.68, 4.56, 4.13, and 5.15% ID/g, respectively, at 2 min) of and fast clearance from the brain. Autoradiography with sections of postmortem AD brain and transgenic mouse brain confirmed the high affinity of these tracers. These preliminary results strongly suggest the dibenzylideneacetone structure to be a potential new scaffold for β-amyloid imaging probes. Topics: Aged; Amyloid beta-Peptides; Animals; Brain; Drug Design; Female; Fluorine Radioisotopes; Humans; Ligands; Male; Mice; Molecular Probes; Pentanones; Peptide Fragments; Plaque, Amyloid; Positron-Emission Tomography; Protein Multimerization; Protein Structure, Secondary; Radiochemistry; Structure-Activity Relationship; Tomography, Emission-Computed, Single-Photon	2011

Article

Year

Synthesis and structure-affinity relationships of novel dibenzylideneacetone derivatives as probes for β-amyloid plaques.

Journal of medicinal chemistry, 2011, Apr-14, Volume: 54, Issue:7

A new and extensive set of dibenzylideneacetone derivatives was synthesized and screened for affinity toward Aβ(1-42) aggregates. Structure-activity relationships revealed the binding of dibenzylideneacetones to be affected by various substituents. The introduction of a substituent group in the ortho position reduced or abolished the binding. However, the para position was highly tolerant of sterically demanding substitutions. Three radioiodinated ligands (6, 70, and 71) and two (18)F fluoro-pegylated (FPEG) ligands (83 and 85) were prepared, all of which displayed high affinity for Aβ(1-42) aggregates (K(i) ranging from 0.9 to 7.0 nM). In biodistribution experiments, they exhibited good initial penetration (1.59, 4.68, 4.56, 4.13, and 5.15% ID/g, respectively, at 2 min) of and fast clearance from the brain. Autoradiography with sections of postmortem AD brain and transgenic mouse brain confirmed the high affinity of these tracers. These preliminary results strongly suggest the dibenzylideneacetone structure to be a potential new scaffold for β-amyloid imaging probes.

Topics: Aged; Amyloid beta-Peptides; Animals; Brain; Drug Design; Female; Fluorine Radioisotopes; Humans; Ligands; Male; Mice; Molecular Probes; Pentanones; Peptide Fragments; Plaque, Amyloid; Positron-Emission Tomography; Protein Multimerization; Protein Structure, Secondary; Radiochemistry; Structure-Activity Relationship; Tomography, Emission-Computed, Single-Photon

2011