Dennis O'Shea, Rabia Ahmad, Erik Årstad, Michelle Avory, Wai-Fung Chau, Clare Durrant, Ella Hirani, Paul A Jones, Imtiaz Khan, Sajinder K Luthra, Dimitrios Mantzilas, Véronique Morisson-Iveson, Joanna Passmore, Edward G Robins, Bo Shan, Harry Wadsworth, Sarah Walton, Yongjun Zhao, William Trigg
A series of novel TSPO ligands based on the tetracyclic class of translocator protein (TSPO) ligands first described by Okubo et al. 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.
April 15, 2013: Bioorganic & Medicinal Chemistry Letters