61652-16-2Relevant academic research and scientific papers
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.
Optimized palladium-based approaches to analogues of PK 11195
Guillou, Sandrine,Janin, Yves L.
experimental part, p. 1377 - 1384 (2009/04/07)
(Chemical Equation Presented) The peripheral-type benzodiazepine receptor ligands such as PK 11195 and Ro 5-4864 were found more than twenty years ago in the course of research on neurobiology. These ligands were instrumental in pointing out an involvement of the peripheral-type benzodiazepine receptor (PBR) in apoptosis processes. With in mind an improvement of the solubility of PK 11195 in biological media, we report here improved reaction conditions for the palladium-based arylation reaction of alkyl 1-bromoisoquinoline-3-carboxylates and its ethyl 4-bromoquinoline-2-carboxylate isomer. The use of [1,1′-bis(diphenylphosphino) ferrocene] dichloropalladium as a precatalyst enabled a much improved preparation of an array of the 1-arylisoquinoline-3- carboxylates as well as 4-arylquinoline-3-carboxylates. This work should pave the way for the design of chemical probes aiming at the elucidation of the PBR biological role(s).
