14080-51-4Relevant articles and documents
A novel series of positive modulators of the AMPA receptor: Discovery and structure based hit-to-lead studies
Jamieson, Craig,Basten, Stephanie,Campbell, Robert A.,Cumming, Iain A.,Gillen, Kevin J.,Gillespie, Jonathan,Kazemier, Bert,Kiczun, Michael,Lamont, Yvonne,Lyons, Amanda J.,MacLean, John K.F.,Moir, Elizabeth M.,Morrow, John A.,Papakosta, Marianthi,Rankovic, Zoran,Smith, Lynn
, p. 5753 - 5756 (2010)
Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22, a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor.
Concise synthesis of tpca-1 and related thiophene-carboxamides by cross coupling
Kawasaki, Norihiko,Fukuda, Hayato,Ishihara, Jun
, p. 707 - 716 (2020/01/31)
A synthesis of 5-substituted 2-[(aminocarbonyl)amino]-3-thiophene-carboxamides is described. The coupling reaction of 2-ureidothiophene-3-carboxamide and various aryl compounds allows the concise approach of promising candidates for IKK-2 inhibitor, such as TPCA-1.
Thiazole formation through a modified Gewald reaction
Mallia, Carl J.,Englert, Lukas,Walter, Gary C.,Baxendale, Ian R.
supporting information, p. 875 - 883 (2015/08/24)
The synthesis of thiazoles and thiophenes starting from nitriles, via a modified Gewald reaction has been studied for a number of different substrates. 1,4-Dithiane-2,5-diol was used as the aldehyde precursor to give either 2-substituted thiazoles or 2-substituted aminothiophenes depending on the substitution of the α-carbon to the cyano group.