Thieno[2,3-d]pyrimidines and -[1,3]oxazines as Glutamate Antagonists and Investigations on the Inhibitory Potency toward Human Leukocyte Elastase

[摘要]：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 mu M) 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 mu M.

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