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

Abstract 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.