ANTIINFLAMMATORY AND ANALGESIC ACTIVITIES OF 3-IMINO-1-OXOISOINDOLINES IN CF1 MICE

A series of 3-imino-1-oxoisoindolines were shown to be potent anti-inf lammatory and analgesic agents at 8 mg/kg, intraperitoneally in mice. The compounds were also able to protect against lipodisaccharide induc ed endotoxic shock and death better than the current clinical agents. These agents appear to function by blocking the release of TNF alpha a nd IL-1 from macrophages as well as competition with their respective high affinity receptors on target tissue, eg, fibroblasts, and macroph ages. In addition lysosomal hydrolytic enzymes were inhibited as well as leukotriene synthesis in macrophages by the agents.