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Blair A, Zmuda F, Malviya G, et al. A novel . Chem Sci. 2015;6(8):4772-4777doi: 10.1039/c5sc01647a.
Blair, A., Zmuda, F., Malviya, G., Tavares, A. A. S., Tamagnan, G. D., Chalmers, A. J., Dewar, D., Pimlott, S. L., & Sutherland, A. (2015). A novel . Chemical science, 6(8), 4772-4777. https://doi.org/10.1039/c5sc01647a
Blair, Adele, et al. "A novel ." Chemical science vol. 6,8 (2015): 4772-4777. doi: https://doi.org/10.1039/c5sc01647a
Blair A, Zmuda F, Malviya G, Tavares AAS, Tamagnan GD, Chalmers AJ, Dewar D, Pimlott SL, Sutherland A. A novel . Chem Sci. 2015 Aug 01;6(8):4772-4777. doi: 10.1039/c5sc01647a. Epub 2015 May 27. PMID: 29142713; PMCID: PMC5667507.
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Chem Sci. 2015 Aug 01;6(8):4772-4777. doi: 10.1039/c5sc01647a. Epub 2015 May 27.

A novel .

Chemical science

Adele Blair, Filip Zmuda, Gaurav Malviya, Adriana A S Tavares, Gilles D Tamagnan, Anthony J Chalmers, Deborah Dewar, Sally L Pimlott, Andrew Sutherland

Affiliations

  1. WestCHEM , School of Chemistry , University of Glasgow , The Joseph Black Building , Glasgow G12 8QQ , UK . Email: [email protected] ; ; Tel: +44 (0)141 330 5936.
  2. Wolfson Whol Cancer Research Centre , Institute of Cancer Sciences , University of Glasgow , Glasgow G61 1QH , UK.
  3. Nuclear Imaging Facility , The Beatson Institute for Cancer Research , Glasgow G61 1BD , UK.
  4. Molecular NeuroImaging, and LLC , 60 Temple Street , New Haven , Connecticut , USA.
  5. Institute of Neuroscience and Psychology , College of Medical , Veterinary and Life Sciences , University of Glasgow , Glasgow G12 8QQ , UK.
  6. West of Scotland Radionuclide Dispensary , University of Glasgow and North Glasgow University Hospital NHS Trust , Glasgow G11 6NT , UK.

PMID: 29142713 PMCID: PMC5667507 DOI: 10.1039/c5sc01647a

Abstract

The translocator protein (TSPO) is an important target for imaging focal neuroinflammation in diseases such as brain cancer, stroke and neurodegeneration, but current tracers for non-invasive imaging of TSPO have important limitations. We present the synthesis and evaluation of a novel 3-fluoromethylquinoline-2-carboxamide, AB5186, which was prepared in eight steps using a one-pot two component indium(iii)-catalysed reaction for the rapid and efficient assembly of the 4-phenylquinoline core. Biological assessment and the implementation of a physicochemical study showed AB5186 to have low nanomolar affinity for TSPO, as well as optimal plasma protein binding and membrane permeability properties. Generation of [

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