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Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.

Bioorganic & medicinal chemistry letters 2006 Mar 1; 16(5):1350-2

Link to PubMed abstract

Chandra R R, Kung M MP, Kung H HF

Department of Radiology, University of Pennsylvania, Room 305, 3700 Market Street, Philadelphia, PA 19104, USA.

Novel 2,5-diphenylthiophene derivatives were synthesized and structure activity relationship with regard to Abeta plaque binding was studied. Binding affinities of these compounds were found to range from 3.9 to >1000 nM, depending on the substitution patterns on the phenyl ring. The fluoroethyl-substituted thiophene derivatives showed excellent binding affinities. These compounds may be useful for the development of novel PET tracers for the imaging of beta-amyloid plaques in the brain of patients with Alzheimer's disease.