title: 2-Arylimidazo[2,1-b]benzothiazoles: a new family of amyloid binding agents with potential for PET and SPECT imaging of Alzheimer's brain.
abstract: We designed and synthesized a small series of 2-aryl-imidazo[2,1-b]benzothiazole, representing a combination of motifs from the two most potent amyloid imaging agents, PIB and IMPY. The binding affinity of the new compounds ranged from 6 to 133 nM. Among the best compounds, 3b (K(i)=6 nM) can be labeled with (11)CH(3) for PET imaging whereas 3j (K(i)=10.9 nM) can be labeled with (123)I for SPECT imaging.
authors: Institute for Neurodegenerative Disorders, 60 Temple St., Suite 8A, New Haven, CT 06510, USA. dalagille@mnimaging.com
authors: David
authors: D
authors: Alagille
authors: Herve
authors: H
authors: DaCosta
authors: Ronald M
authors: RM
authors: Baldwin
authors: Gilles D
authors: GD
authors: Tamagnan
mesh_terms: D000544:Alzheimer Disease / Q000175:diagnosis*; D000682:Amyloid / Q000737:chemistry / Q000378:metabolism; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000737:chemistry; D001667:Binding, Competitive; D001681:Biological Assay; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry; D049268:Positron-Emission Tomography; D011485:Protein Binding; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D000682:Amyloid; D052160:Benzothiazoles; D007093:Imidazoles; C005465:benzothiazole