Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.

Corey Hopkins,Kent Neuenschwander,Anthony Scotese,Sharon Jackson,Thaddeus Nieduzak,Henry Pauls,Guyan Liang,Keith Sides,Dona Cramer,Jennifer Cairns,Sebastien Maignan,Magali Mathieu

Bioorganic & Medicinal Chemistry Letters（2004）

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摘要

In this manuscript, the synthesis and SAR evaluation of a novel pyrazinone class of tryptase inhibitors is described. Chemical optimization of the P1 and P4 groups led to the identification of 7p (Ki=93nM) as a potent inhibitor of mast cell tryptase.

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关键词

Mast cell tryptase,SAR,Pyrazinone

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