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Bioorg Med Chem Lett. 2012 Sep 15;22(18):5795-800. doi: 10.1016/j.bmcl.2012.07.093. Epub 2012 Aug 3.

Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein--potential novel positron emitting tomography imaging agents.

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GE Healthcare, The Grove Centre, White Lion Road, Amersham, Bucks HP7 9LL, UK.


A series of novel ligands based on the diaryl anilide (DAA) class of translocator protein (TSPO) ligands was synthesised and evaluated as potential positron emitting tomography (PET) ligands for imaging TPSO in vivo. Fluorine-18 labelling of the molecules was achieved using direct radiolabelling or synthon based labelling approaches. Several of the ligands prepared have promising profiles as potential TSPO PET imaging ligands and will be evaluated further as potential clinical imaging agents.

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