Development of the First Two-Pore Domain Potassium Channel TWIK-Related K<sup>+</sup> Channel 1-Selective Agonist Possessing in Vivo Antinociceptive Activity
作者:Delphine Vivier、Ismail Ben Soussia、Nuno Rodrigues、Stéphane Lolignier、Maïly Devilliers、Franck C. Chatelain、Laetitia Prival、Eric Chapuy、Geoffrey Bourdier、Khalil Bennis、Florian Lesage、Alain Eschalier、Jérôme Busserolles、Sylvie Ducki
DOI:10.1021/acs.jmedchem.6b01285
日期:2017.2.9
development of a novel class of analgesic drugs, suggesting that activation of TREK-1 could result in pain inhibition. Here, we report the synthesis of a series of substitutedacrylicacids (1–54) based on our previous work with caffeate esters. The analogues were evaluated for their ability to modulate TREK-1 channel by electrophysiology and for their in vivo antinociceptive activity (acetic acid-induced
Hierarchically Pore Structure poly 2-(Dimethyl amino) ethyl methacrylate/Hi-ZSM-5: A Novel Acid–Base Bi-functional Catalyst as Heterogeneous Platform for a Tandem Reaction
作者:Roozbeh Javad Kalbasi、Anahita Khojastegi
DOI:10.1007/s10562-018-2301-z
日期:2018.3
A simple method is developed to prepare an efficient and low cost acid–base bifunctional catalyst by using poly 2-(dimethyl amino) ethyl methacrylate as a basic part and hierarchical ZSM-5 as an acidic part of the catalyst. Tandemreaction of deacetalization–Knoevenagel condensation was selected to evaluate the prepared catalyst and the outcomes were excellent.Graphical Abstract