2401-97-0Relevant academic research and scientific papers
Late stage iodination of biologically active agents using a one-pot process from aryl amines
Sloan, Nikki L.,Luthra, Sajinder K.,McRobbie, Graeme,Pimlott, Sally L.,Sutherland, Andrew
, p. 54881 - 54891 (2017/12/12)
A simple and effective one-pot tandem procedure that generates aryl iodides from readily available aryl amines via stable diazonium salts has been developed. The operationally simple procedure and mild conditions allow late-stage iodination of a wide range of aryl compounds bearing various functional groups and substitution patterns. A novel synthetic strategy involving the preparation of nitroaryl compounds followed by a chemoselective tin(ii) dichloride reduction and the use of the one-pot diazotisation-iodination transformation was also developed. The general applicability of this approach was demonstrated with the preparation of a number of medicinally important compounds including CNS1261, a SPECT imaging agent of the N-methyl-d-aspartate (NMDA) receptor and IBOX, a compound used to detect amyloid plaques in the brain.
Structure-activity relationships of novel iodinated quinoline-2- carboxamides for targeting the translocator protein
Blair, Adele,Stevenson, Louise,Dewar, Deborah,Pimlott, Sally L.,Sutherland, Andrew
supporting information, p. 1461 - 1466 (2013/11/19)
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.
New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein
Stevenson, Louise,Tavares, Adriana A.S.,Brunet, Aurelie,McGonagle, Fiona I.,Dewar, Deborah,Pimlott, Sally L.,Sutherland, Andrew
supporting information; experimental part, p. 954 - 957 (2010/06/11)
With the aim of developing new SPECT imaging agents for the translocator protein (TSPO), a small library of iodinated quinoline-2-carboxamides have been prepared and tested for binding affinity with TSPO. N,N-Diethyl-3-iodomethyl-4-phenylquinoline-2-carboxamide was found to have excellent affinity (Ki 12.0 nM), comparable to that of the widely used TSPO imaging agent PK11195.
