23837-10-7Relevant articles and documents
Synthesis and pharmacological characterisation of arctigenin analogues as antagonists of AMPA and kainate receptors
Butts, Craig P.,Collingridge, Graham L.,Jane, David E.,Mallah, Shahida,Molnár, Elek,Re?nik, Lisa-Maria,Thatcher, Robert J.,Willis, Christine L.
supporting information, p. 9154 - 9162 (2021/11/16)
(-)-Arctigenin and a series of new analogues have been synthesised and then tested for their potential as AMPA and kainate receptor antagonists of human homomeric GluA1 and GluK2 receptors expressed in HEK293 cells using a Ca2+ influx assay. In general, these compounds showed antagonist activity at both receptors with greater activity evident at AMPARs. Schild analysis indicates that a spirocyclic analogue 6c acts as a non-competitive antagonist. Molecular docking studies in which 6c was docked into the X-ray crystal structure of the GluA2 tetramer suggest that (-)-arctigenin and its analogues bind in the transmembrane domain in a similar manner to the known AMPA receptor non-competitive antagonists GYKI53655 and the antiepileptic drug perampanel. The arctigenin derivatives described herein may serve as novel leads for the development of drugs for the treatment of epilepsy. This journal is
Visible-Light Photoredox-Catalyzed Thioacetalization of Aldehydes Under Metal-Free and Solvent-Free Conditions
Du, Kai,Wang, Shao-Chien,Basha, R. Sidick,Lee, Chin-Fa
, p. 1597 - 1605 (2018/12/11)
A first visible-light photoredox-catalyzed thioacetalization of aldehydes under metal-free and solvent-free conditions is described. Under blue LED irradiation, a reactive thiyl radical was initially generated through single-electron oxidation of thiol, w
Reduction of titanocene dichloride with dysprosium: Access to a stable titanocene(II) equivalent for phosphite-free Takeda carbonyl olefination
Bousrez,Déchamps,Vasse,Jaroschik
supporting information, p. 9359 - 9362 (2015/06/16)
The reduction of titanocene dichloride with dysprosium yields a new titanocene(ii) equivalent without the need for further stabilising ligands. This reagent can be employed in combination with dithioacetals for the olefination of different carbonyl groups and allows for a simplified all-in-one procedure.