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Issue 11, 2013
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Structure–activity relationships of novel iodinated quinoline-2-carboxamides for targeting the translocator protein

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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.

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

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Publication details

The article was received on 03 Sep 2013, accepted on 16 Sep 2013 and first published on 17 Sep 2013


Article type: Concise Article
DOI: 10.1039/C3MD00249G
Med. Chem. Commun., 2013,4, 1461-1466

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

    A. Blair, L. Stevenson, D. Dewar, S. L. Pimlott and A. Sutherland, Med. Chem. Commun., 2013, 4, 1461
    DOI: 10.1039/C3MD00249G

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