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  • Title: Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
    Author: Chandra R, Kung MP, Kung HF.
    Journal: Bioorg Med Chem Lett; 2006 Mar 01; 16(5):1350-2. PubMed ID: 16325402.
    Abstract:
    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.
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