958641-75-3

Upstream product

• 958641-74-2 2-[4-(2-hydroxyethoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine 
• 813-19-4 bis(tri-n-butyltin) 
• 958641-87-7 2-[4-(2-t-butyldiphenylsiloxyethoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine 
• 20511-12-0 2-amino-5-iodopyridine 
• 2491-38-5 2-bromo-1-(4'-hydroxyphenyl)-1-ethanone 
• 956499-76-6 2-(4-hydroxyphenyl)-6-iodoimidazo[1,2-a]pyridine 

Downstream Products

• 958641-76-4 2-[4'-(2''-hydroxyethoxy)phenyl]-6-[123I]iodoimidazo[1,2-a]pyridine 

Relevant academic research and scientific papers

Design, Synthesis, and Preliminary Evaluation of SPECT Probes for Imaging β-Amyloid in Alzheimer's Disease Affected Brain

In this study, we synthesized of a series of 2-phenyl- and 2-pyridyl-imidazo[1,2-a]pyridine derivatives and examine their suitability as novel probes for single-photon emission computed tomography (SPECT)-based imaging of β-amyloid (Aβ). Among the 11 evaluated compounds, 10 showed moderate affinity to Aβ(1-42) aggregates, exhibiting half-maximal inhibitory concentrations (IC50) of 14.7 ± 6.07-87.6 ± 39.8 nM. In vitro autoradiography indicated that 123I-labeled triazole-substituted derivatives displayed highly selective binding to Aβ plaques in the hippocampal region of Alzheimer's disease (AD)-affected brain. Moreover, biodistribution studies performed on normal rats demonstrated that all 123I-labeled probes featured high initial uptake into the brain followed by a rapid washout and were thus well suited for imaging Aβ plaques, with the highest selectivity observed for a 1H-1,2,3-triazole-substituted 2-pyridyl-imidazopyridine derivative, [123I]ABC577. This compound showed good kinetics in rat brain as well as moderate in vivo stability in rats and is thus a promising SPECT imaging probe for AD in clinical settings.

UTILIZATION OF NOVEL COMPOUNDS WITH AMYLOID AFFINITY AND METHOD OF PRODUCING THE SAME

The invention provides a reagent for detecting amyloid deposited in a biological tissue which can detect amyloid in vitro and in vivo with high sensitivity using a compound which has affinity with amyloid and is suppressed in toxicity such as mutagencity. The reagent for detecting amyloid deposited in a biological tissue comprises a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent carbon or nitrogen; R1 is a radioactive halogen substituent; R2 is a group selected from the group consisting of hydrogen, hydroxyl group, methoxy group, carboxyl group, amino group, N-methylamino group, N,N-dimethylamino group and cyano group; and m is an integer of 0 to 2, provided that at least one of A1, A2, and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 and A4.

NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID

The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.