204850-15-7Relevant academic research and scientific papers
ANTI-VIRAL COMPOUNDS
-
, (2008/12/08)
Compounds effective in inhibiting replication of Hepatitis C virus ( HCV ) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, coformulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease
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.
, p. 1060 - 1067 (2007/10/03)
A series of 2-amino-4H-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- iodophenyl)amino]benz[d][1,3]oxazin-4-one (37) show improved potency compared to the reference compound FUT-175. Many of these active compounds also possess increased selectivity for C1r compared to trypsin and enhanced hydrolytic stability relative to 2-(2-iodophenyl)-4H-3,1-benzoxazin-4-one (1).
