Radiolabeled bioactive benzoheterocycles for imaging β-amyloid plaques in Alzheimer's disease

• Published in: European journal of medicinal chemistry 2014-11, Vol.87, p.703-721
• Main Authors: Yang, Yanping, Cui, Mengchao
• Format: Article
• Language: English
• Subjects: Alzheimer Disease - diagnostic imaging; Alzheimer's disease; Benzoheterocycles; Heterocyclic Compounds - administration & dosage; Humans; Imaging agents; Plaque, Amyloid - diagnostic imaging; Positron-Emission Tomography; Radiolabeled; Tomography, Emission-Computed, Single-Photon; β-amyloid plaque
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2014.10.012

Alzheimer's disease (AD) is a debilitating neurodegenerative dementia that involves substantial neuronal loss. Extracellular deposition of neurotoxic β-amyloid (Aβ) plaques in the brain has been recognized as the central histological characteristic of AD. In the past decade, precise detection of the Aβ plaques at preclinical AD with positron emission tomography (PET) or single photon emission computed tomography (SPECT) has achieved continued development. A big category of Aβ imaging agents was benzoheterocycles which derived from Thioflavin-T (ThT), a traditional amyloid binding dye. This review summarizes the past and current status of radioactive benzoheterocycles designed to selectively bind to Aβ plaques. Separate sections discuss the chemical synthesis, in vitro and in vivo investigations of radiolabeled benzothiazole, benzoxazole, benzofuran, benzothiophene, indole, imidazopyridine and quinoxaline analogs to act as PET/SPECT candidates for imaging Aβ plaques. [Display omitted] •We summarized the progress of radiolabeled benzoheterocycles for imaging Aβ plaques.•Synthetic approaches, binding potencies and brain pharmacokinetics were discussed.•According to the type of scaffolds, the discussion was made in divided sections.