In 2019,ACS Chemical Neuroscience included an article by Pallesen, Jakob; Moellerud, Stine; Frydenvang, Karla; Pickering, Darryl S.; Bornholdt, Jan; Nielsen, Birgitte; Pasini, Diletta; Han, Liwei; Marconi, Laura; Kastrup, Jette Sandholm; Johansen, Tommy N.. Electric Literature of C4H5ClO3. The article was titled 《N1-substituted quinoxaline-2,3-diones as kainate receptor antagonists: x-ray crystallography, structure-affinity relationships, and in vitro pharmacology》. The information in the text is summarized as follows:
Among the ionotropic glutamate receptors, the physiol. role of kainate receptors is less well understood. Although ligands with selectivity toward the kainate receptor subtype GluK1 are available, tool compounds with selectivity at the remaining kainate receptor subtypes are sparse. Here, we have synthesized a series of quinoxaline-2,3-diones with substitutions in the N1-, 6-, and 7-position to investigate the structure-activity relationship (SAR) at GluK1-3 and GluK5. Pharmacol. characterization at native and recombinant kainate and AMPA receptors revealed that I had a GluK3-binding affinity (Ki) of 0.142 μM and 8-fold preference for GluK3 over GluK1. Despite lower binding affinity of II at GluK3 (Ki = 2.91 μM), its preference for GluK3 over GluK1 and GluK2 was >30-fold. I was crystallized with the GluK1 ligand-binding domain to understand the SAR. The X-ray structure showed that I stabilized the protein in an open conformation, consistent with an antagonist binding mode. In the experimental materials used by the author, we found Ethyl oxalyl monochloride(cas: 4755-77-5Electric Literature of C4H5ClO3)
Ethyl oxalyl monochloride(cas: 4755-77-5) belongs to acyl chlorides. In the laboratory, acyl chlorides are generally prepared by treating carboxylic acids with thionyl chloride (SOCl2). The reaction is catalyzed by dimethylformamide and other additives.Electric Literature of C4H5ClO3
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