Anti-inflammatory and analgesic activities of 3-imino-1-oxoisoindolines in CF1 mice

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