Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors

A series of 2-aryl-4H-3,1-benzoxazin-4-ones have been synthesized and tested for inhibitory activity against C1r serine protease. Compounds were found that were equipotent and more selective than the reference compound FUT-175. A series of 2-aryl-4H-3,1-benzoxazin-4-ones (A) have been synthesized an...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1996-03, Vol.6 (6), p.679-682
Main Authors: Gilmore, John L., Hays, Sheryl J., Caprathe, Bradley W., Lee, Chitase, Emmerling, Mark R., Michael, Walter, Jaen, Juan C.
Format: Article
Language:English
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Summary:A series of 2-aryl-4H-3,1-benzoxazin-4-ones have been synthesized and tested for inhibitory activity against C1r serine protease. Compounds were found that were equipotent and more selective than the reference compound FUT-175. A series of 2-aryl-4H-3,1-benzoxazin-4-ones (A) have been synthesized and tested for inhibitory activity against C1r serine protease. Compounds were found that were equipotent and more selective than the reference compound FUT-175.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(96)00094-7