Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter

Jobson, N., Crawford, A., Dewar, D., Pimlott, S. and Sutherland, A. (2009) Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorganic and Medicinal Chemistry Letters, 19(17), pp. 4996-4998. (doi: 10.1016/j.bmcl.2009.07.064)

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Abstract

A stereoselective 10-step synthesis of iodophenoxy analogues of (2R,3S)-reboxetine has been developed with the aim of generating a new SPECT imaging agent for the noradrenaline transporter (NAT). In vitro testing of these compounds against various mono-amine transporters showed an ortho-iodophenoxy analogue to have excellent affinity (Ki 8.4 nM) and good selectivity for NAT.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Dewar, Dr Deborah and Pimlott, Dr Sally and Sutherland, Professor Andrew
Authors: Jobson, N., Crawford, A., Dewar, D., Pimlott, S., and Sutherland, A.
College/School:College of Medical Veterinary and Life Sciences > Institute of Neuroscience and Psychology
College of Science and Engineering > School of Chemistry
Journal Name:Bioorganic and Medicinal Chemistry Letters
ISSN:0960-894X

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