Design, synthesis, and biological activity of diiminoisoindolines as complement component 3a antagonists

The failure to fully regulate the inflammation response has been linked to diseases such as rheumatoid arthritis, septic shock syndrome, and asthma. T he human complement system initiates and regulates the inflammation respons e through a cascade of regulatory factors, Complement Component 3a (C3a) is an essential regulatory factor and inhibiting its binding to a C3a recepto r will diminish the inflammation response by disrupting the cascade. We rep ort the design, synthesis, in vitro and in vivo activity of diiminoisoindol ines as C3a antagonists. (C) 2001 Elsevier Science Ltd. All rights reserved .