1217864-83-9Relevant academic research and scientific papers
Thieno[2,3-d]pyrimidines and -[1,3]oxazines as glutamate antagonists and investigations on the inhibitory potency toward human leukocyte elastase
Briel, Detlef,Rybak, Anastasiya,Kronbach, Christiane,Unverferth, Klaus,Gonzalez Tanarro, Camino M.,Guetschow, Michael
experimental part, p. 634 - 639 (2010/08/20)
(Chemical Equation Presented) A series of fused thiophene derivatives, that is, representatives of thieno[2,3-d]pyrimidines, thieno[2,3-d][1,3]oxazines and thieno[2,3-d][1,3]thiazines, with the common 5-methyl-6-phenyl substitution pattern was synthesized. The target compounds, e.g., 7 or 8, were designed as cyclic analogs of ethyl 2-amino-4-methyl-5-phenylthiophene-3-carboxylate, an antagonist at the GluR6 kainate receptor. Thieno[2,3-d][1,3]oxazin-4-one 2 (R = C2H5) was identified as new a potent inhibitor (IC50 = 17 lM) of this receptor subtype. The inhibitory potency of 2 (R = C2H5) against human leukocyte elastase was also examined. The compound was characterized as a noncovalent inhibitor with an IC50 value of 8.8 μM.
