39959-51-8Relevant articles and documents
Structure and Reactivity of N-Heterocyclic Alkynyl Hypervalent Iodine Reagents
Le Du, Eliott,Duhail, Thibaut,Wodrich, Matthew D.,Scopelliti, Rosario,Fadaei-Tirani, Farzaneh,Anselmi, Elsa,Magnier, Emmanuel,Waser, Jerome
supporting information, p. 10979 - 10986 (2021/06/08)
Ethynylbenziodoxol(on)e (EBX) cyclic hypervalent iodine reagents have become popular reagents for the alkynylation of radicals and nucleophiles, but only offer limited possibilities for further structure and reactivity fine-tuning. Herein, the synthesis o
Synthesis of N-Heteroaromatic Compounds through Cyclocarbonylative Sonogashira Reactions
Aronica, Laura Antonella,Albano, Gianluigi,Giannotti, Luca,Meucci, Elisa
supporting information, p. 955 - 963 (2017/02/15)
A protocol based on cyclocarbonylative Sonogashira reactions has been developed for the synthesis of nitrogen-containing heterocycles. The process is carried out under CO pressure, in the presence of a small amount of PdCl2(PPh3)sub
Synthesis, in vitro and in vivo evaluation, and radiolabeling of aryl anandamide analogues as candidate radioligands for in vivo imaging of fatty acid amide hydrolase in the brain
Wyffels, Leonie,Muccioli, Giulio G.,De Bruyne, Sylvie,Moerman, Lieselotte,Sambre, Johan,Lambert, Didier M.,De Vos, Filip
supporting information; experimental part, p. 4613 - 4622 (2010/02/28)
Fatty acid amide hydrolyase (FAAH) is one of the main enzymes responsible for terminating the signaling of endocannabinoids in the brain. Imaging FAAH in vivo using PET or SPECT is important to deeper understanding of its role in neuropsychiatric disorders. However, at present, no radioligand is available for mapping the enzyme in vivo. Here, we synthesized 18 aryl analogues of anandamide, FAAH's endogenous substrate, and in vitro evaluated their potential as metabolic trapping tracers. Interaction studies with recombinant FAAH revealed good to very good interaction of the methoxy substituted aryl anandamide analogues 17, 18, 19, and 20 with FAAH and they were identified as competing substrates. Compounds 17 and 18 did not display significant binding to CB1 and CB2 cannabinoid receptors and stand out as potential candidate metabolic trapping tracers. They were successfully labeled with 11C in good yields and high radiochemical purity and displayed brain uptake in C57BL/6J mice. Radioligands [11C]-17 and [ 11C]-18 merit further investigation in vivo.
