104598-91-6Relevant academic research and scientific papers
Thermal and spectroscopic studies of 2,3,5-trisubstituted and 1,2,3,5-tetrasubstituted indoles as non-competitive antagonists of GluK1/GluK2 receptors
Bartyzel, Agata,Kaczor, Agnieszka A.,G?uchowska, Halina,Pitucha, Monika,Wróbel, Tomasz M.,Matosiuk, Dariusz
, p. 935 - 944 (2018)
This paper reports the thermal stability and thermal degradation of six derivatives of indole by means of TG-DSC (in air) and TG-FTIR (in nitrogen) techniques. The compounds were also characterized by infrared spectroscopy. In addition, IR spectra were ca
Structural studies, homology modeling and molecular docking of novel non-competitive antagonists of GluK1/GluK2 receptors
Kaczor, Agnieszka A.,Karczmarzyk, Zbigniew,Fruziński, Andrzej,Pihlaja, Kalevi,Sinkkonen, Jari,Wiin?maki, Kirsti,Kronbach, Christiane,Unverferth, Klaus,Poso, Antti,Matosiuk, Dariusz
, p. 787 - 795 (2014/01/23)
Non-competitive ligands of kainate receptors have focused significant attention as medicinal compounds because they seem to be better tolerated than competitive antagonists and uncompetitive blocker of these receptors. Here we present structural studies (
Novel non-competitive antagonists of kainate GluK1/GluK2 receptors
Kaczor, Agnieszka Anna,Kronbach, Christiane,Unverferth, Klaus,Pihlaja, Kalevi,Wiinam?ki, Kirsti,Sinkkonen, Jari,Kijkowska-Murak, Urszula,Wróbel, Tomasz,Stacha, Tomasz,Matosiuk, Dariusz
, p. 891 - 898 (2013/02/22)
A series of 2,3,5-trisubstituted and 1,2,3,5-tetrasubstituted indoles is synthesized by Fisher or Bischler method, followed by alkylation with an appropriate alkyl or aryl halide. Two compounds exhibit non-competitive antagonism towards GluK1 and six - towards GluK2 receptor. The values of IC 50 are in micromolar range. The investigated compounds belong to the most active GluK1 non-competitive inhibitors and are the first known negative allosteric modulators of GluK2 receptor. The observed pattern of activity is rationalized by molecular modelling, in particular by construction of the pharmacophore model.
