title: Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
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.
authors.affiliation: Department of Radiology, University of Pennsylvania, Room 305, 3700 Market Street, Philadelphia, PA 19104, USA.
authors.forename: Rajesh
authors.initials: R
authors.lastname: Chandra
authors.forename: Mei-Ping
authors.initials: MP
authors.lastname: Kung
authors.forename: Hank F
authors.initials: HF
authors.lastname: Kung
mesh_terms: D000544:Alzheimer Disease / Q000175:diagnosis / Q000378:metabolism*; D016229:Amyloid beta-Peptides / Q000032:analysis / Q000378:metabolism*; D000818:Animals; D002460:Cell Line; D015195:Drug Design; D008024:Ligands; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D016229:Amyloid beta-Peptides; D008024:Ligands; D013876:Thiophenes