902453-94-5Relevant academic research and scientific papers
Synthesis and structure-affinity relationships of new 4-(6-iodo-H- imidazo[1,2-a]pyridin-2-yl)-N-dimethylbenzeneamine derivatives as ligands for human β-amyloid plaques
Cai, Lisheng,Cuevas, Jessica,Temme, Sebastian,Herman, Mary M.,Dagostin, Claudio,Widdowson, David A.,Innis, Robert B.,Pike, Victor W.
, p. 4746 - 4758 (2007)
A new and extensive set of 4-(6-iodo-H-imidazo[1,2-a]pyridin-2-yl)-N- dimethylbenzeneamine (IMPY) derivatives was synthesized and assayed for affinity toward human Aβ plaques. 6-Ethylthio- (12h), 6-cyano-(12e), 6-nitro- (12f), and 6-p-methoxybenzylthio- (15d) analogues were discovered to have high affinity (KI I = 7.4 nM) whereas a methyl substituent did not (14c). The tolerance for nonhydrophilic thioether substituents in the 6-position opens up the possibility of developing new sensitive positron emission tomography radioligands for imaging human Aβ plaques in Alzheimer's disease, especially in view of the amenability of thioethers to be labeled with carbon-11 or fluorine-18 through S-alkylation reactions. The structure-activity relationships revealed in this study extends insight into the topography of the binding site for IMPY-like ligands in human Aβ plaques.
BETA-AMYLOID PET IMAGING AGENTS
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Page/Page column 17, (2008/06/13)
Novel derivatives of imidazopyridinylbenzeneamines and novel derivatives of benzothiazolylbenzeneamines are disclosed that offer improved behavior when used as imaging agents for positron emission tomography of beta-amyloids. Also disclosed is a palladium-catalyzed reaction scheme under microwave conditions for aryl thioethers in general that provides a high ratio of substitution relative to reduction and can be used for the imidazopyridinylbenzeneamine derivatives as well as other compounds of related structure.
