Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4- ones and benzthiazin-4-ones as inhibitors of complement C1r protease

Article abstract of DOI:10.1016/S0960-894X(99)00095-5

A series of 2-sulfonyl-4H-3,1-benzoxazinones was prepared that inhibit C1r protease in vitro. Several compounds were found to be selective for C1r verses the related serine protease trypsin. Selected compounds demonstrated functional activity in a hemolysis assay.