Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
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.
Chandra
Rajesh
R
Department of Radiology, University of Pennsylvania, Room 305, 3700 Market Street, Philadelphia, PA 19104, USA.
Kung
Mei-Ping
MP
Kung
Hank F
HF
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*
D016229:Amyloid beta-Peptides; D008024:Ligands; D013876:Thiophenes