Synthesis of Novel Apocynin Dimer Derivatives

Nicotinamide adenine dinucleotide phosphate (NADPH) oxidase has been proved to be a target of anti-oxidation and anti-inflammation therapy. Apocynin dimer (diapocynin), converted from apocynin by peroxidase-mediated oxidation in vivo, was reported to confer stronger inhibition to NADPH oxidase than apocynin. However, there was limited information about the structural modification of diapocynin. In order to improve the bioactivity of dimeric apocynin, JJA-D0, an apocynin dimer analogue of more functional groups than diapocynin for structural modification, was synthesized in our lab. 14 apocynin dimer derivatives were designed and synthesized on the basis of chemical structure of JJA-D0, attempting to attain more efficient lead compounds for further development.