Structure–activity relationships of novel iodinated quinoline-2-carboxamides for targeting the translocator protein

Blair, A., Stevenson, L., Dewar, D. , Pimlott, S.L. and Sutherland, A. (2013) Structure–activity relationships of novel iodinated quinoline-2-carboxamides for targeting the translocator protein. MedChemComm, 4(11), pp. 1461-1466. (doi: 10.1039/c3md00249g)

Abstract

In an effort to develop a new SPECT imaging agent for the translocator protein (TSPO), a series of novel iodinated quinoline-2-carboxamides have been synthesised and evaluated for binding affinity using rat brain homogenates. The outcome of the biological testing in combination with HPLC determination of the physicochemical properties of these compounds directed the design of new analogues resulting in 4-(2-iodophenyl)quinoline-2-N-diethylcarboxamide, a new TSPO ligand with higher affinity than the widely used clinical imaging agent PK11195.

• Item Type: Articles
• Status: Published
• Refereed: Yes
• Glasgow Author(s) Enlighten ID: Pimlott, Dr Sally and Stevenson, Miss Louise and Dewar, Dr Deborah and Sutherland, Professor Andrew
• Authors: Blair, A., Stevenson, L., Dewar, D., Pimlott, S.L., and Sutherland, A.
• College/School: College of Medical Veterinary and Life Sciences > School of Psychology & Neuroscience; College of Medical Veterinary and Life Sciences > School of Medicine, Dentistry & Nursing; College of Science and Engineering > School of Chemistry
• Journal Name: MedChemComm
• Publisher: Royal Society of Chemistry
• ISSN: 2040-2503
• ISSN (Online): 2040-2511