Aliskiren Copper(II) Complex. Synthesis and Antioxidant Activity

Aliskiren (Alk) is a highly selective competitive inhibitor of renin used for the treatment of hypertension and related cardiovascular diseases. With the aim of improving its biological properties by the strategy of the induction of favorable conformational changes, we designed a metal -based drug. In this work we report the synthesis of a solid copper(II) complex with aliskiren, CuAlk, and its characterization in solution and solid-state. Moreover, and based on the association of hypertension with elevated levels of reactive oxygen species (ROS), the antioxidant properties of CuAlk were studied measuring the activities against 2,2-diphenyl-1-picrilhidrazil (DPPH center dot), hydroxyl (OH center dot) and peroxyl (ROO center dot) radicals, in addition to its superoxide dismutase (SOD) simil activity. Both the ligand and the complex were able to scavenge hydroxyl radicals, but upon complexation, the SOD mimetic activity of the ligand is enhanced.