Literature DB >> 20579877

Use of 2-[(18)F]fluoroethylazide for the Staudinger ligation - Preparation and characterisation of GABA(A) receptor binding 4-quinolones.

Alessandra Gaeta1, John Woodcraft, Stuart Plant, Julian Goggi, Paul Jones, Mark Battle, William Trigg, Sajinder K Luthra, Matthias Glaser.   

Abstract

The labelling reagent 2-[(18)F]fluoroethylazide was used in a traceless Staudinger ligation. This reaction was employed to obtain the GABA(A) receptor binding 6-benzyl-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid (2-[(18)F]fluoroethyl) amide. The radiotracer was prepared with a non-decay corrected radiochemical yield of 7%, a radiochemical purity >95% and a specific radioactivity of 0.9 GBq/micromol. The compound showed low brain penetration in normal rats. A series of fluoroalkyl 4-quinolone analogues with nanomolar to sub-nanomolar affinity for the GABA(A) receptor has been prepared as well. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20579877     DOI： 10.1016/j.bmcl.2010.05.106

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Highly efficient click labeling using 2-[¹⁸F]fluoroethyl azide and synthesis of an ¹⁸FN-hydroxysuccinimide ester as conjugation agent.

Authors:  Dong Zhou; Wenhua Chu; Carmen S Dence; Robert H Mach; Michael J Welch
Journal:  Nucl Med Biol       Date:  2012-07-04       Impact factor: 2.408

Review 2.  Fluorine-18 patents (2009-2015). Part 1: novel radiotracers.

Authors:  Allen F Brooks; Lindsey R Drake; Megan N Stewart; Brian P Cary; Isaac M Jackson; Dale Mallette; Andrew V Mossine; Peter J H Scott
Journal:  Pharm Pat Anal       Date:  2015-12-16

Review 3.  Click Chemistry and Radiochemistry: The First 10 Years.

Authors:  Jan-Philip Meyer; Pierre Adumeau; Jason S Lewis; Brian M Zeglis
Journal:  Bioconjug Chem       Date:  2016-11-22       Impact factor: 4.774

Review 4.  The growing impact of bioorthogonal click chemistry on the development of radiopharmaceuticals.

Authors:  Dexing Zeng; Brian M Zeglis; Jason S Lewis; Carolyn J Anderson
Journal:  J Nucl Med       Date:  2013-04-24       Impact factor: 10.057

Review 5.  Fluorine-18 radiochemistry, labeling strategies and synthetic routes.

Authors:  Orit Jacobson; Dale O Kiesewetter; Xiaoyuan Chen
Journal:  Bioconjug Chem       Date:  2014-12-12       Impact factor: 4.774

Review 6.  Allosteric GABAA Receptor Modulators-A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility.

Authors:  Blanca Angelica Vega Alanis; Maria Teresa Iorio; Luca L Silva; Konstantina Bampali; Margot Ernst; Michael Schnürch; Marko D Mihovilovic
Journal:  Molecules       Date:  2020-02-24       Impact factor: 4.927
  6 in total

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