title: Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.
abstract: 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.
authors: Department of Chemistry, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
authors: J S
authors: JS
authors: Plummer
authors: C
authors: C
authors: Cai
authors: S J
authors: SJ
authors: Hays
authors: J L
authors: JL
authors: Gilmore
authors: M R
authors: MR
authors: Emmerling
authors: W
authors: W
authors: Michael
authors: L S
authors: LS
authors: Narasimhan
authors: M D
authors: MD
authors: Watson
authors: K
authors: K
authors: Wang
authors: R
authors: R
authors: Nath
authors: L M
authors: LM
authors: Evans
authors: J C
authors: JC
authors: Jaen
mesh_terms: D000818:Animals; D003174:Complement C1 Inactivator Proteins / Q000138:chemical synthesis*; D015923:Complement C1r / Q000037:antagonists & inhibitors; D004912:Erythrocytes / Q000187:drug effects; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008956:Models, Chemical; D012756:Sheep; D013449:Sulfonamides / Q000138:chemical synthesis*; D000096926:Benzenesulfonamides
chemical_list: D003174:Complement C1 Inactivator Proteins; D015923:Complement C1r; D013449:Sulfonamides; D000096926:Benzenesulfonamides