Thieno[2,3-d]pyrimidines and -[1,3]oxazines as glutamate antagonists and investigations on the inhibitory potency toward human leukocyte elastase.

Autor:	Briel, Detlef, Rybak, Anastasiya, Kronbach, Christiane, Unverferth, Klaus, González Tanarro, Camino M., Gütschow, Michael
Předmět:	PYRIMIDINES GLUTAMIC acid LEUCOCYTE elastase THIOPHENES THIAZINES HETEROCYCLIC compounds
Zdroj:	Journal of Heterocyclic Chemistry; May2010, Vol. 47 Issue 3, p634-639, 6p, 2 Diagrams, 1 Chart, 1 Graph
Abstrakt:	A series of fused thiophene derivatives, that is, representatives of thieno[2,3-d]pyrimidines, thieno[2,3-d][13]oxazines and thieno[2,3-d][13]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][13]oxazin-4-one 2 (R = C2H5) was identified as new a potent inhibitor (IC50 = 17 μM) 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. J. Heterocyclic Chem., (2010). [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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