2-Amino-4 H-3, 1-benzoxazin-4-ones as inhibitors of C1r serine protease

…, MR Emmerling, W Michael, R Nadimpalli…

Index: Hays, Sheryl J.; Caprathe, Bradley W.; Gilmore, John L.; Amin, Nilam; Emmerling, Mark R.; Michael, Walter; Nadimpalli, Ravi; Nath, Rathna; Raser, Kadee J.; Stafford, Daniel; Watson, Desiree; Wang, Kevin; Jaen, Juan C. Journal of Medicinal Chemistry, 1998 , vol. 41, # 7 p. 1060 - 1067

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Citation Number: 98

Abstract

A series of 2-amino-4 H-3, 1-benzoxazin-4-ones have been synthesized and evaluated as inhibitors of the complement enzyme C1r. C1r is a serine protease at the beginning of the complement cascade, and complement activation by β-amyloid may represent a major contributing pathway to the neuropathology of Alzheimer's disease. Compounds such as 7- chloro-2-[(2-iodophenyl) amino] benz [d][1, 3] oxazin-4-one (32) and 7-methyl-2-[(2- ...