The most advantage of the macrocyclic polyamines is their unique capacity to bind some biologically important metals (Zn, Cu, Co, Fe) and their role was dramatically increased as behaviour models for enzymes and other metalloproteins. The modification of macrocyclic polyamine receptor molecules with additional ligands (arms) enables to interact with nucleobase, sugar and other biomolecules moieties for a more efficient multipoint recognition, as well as for thermodynamic stabilization of the ternary complexes in aqueous solution. Cyclen, cyclam, their derivatives and metallo complexes are proposed as good candidates to cross blood-brain barrier and with low toxicity as potential neuroprotective or neurorescue agents in the treatment of Alzheimer’s disease. In addition, cyclen derivatives showed antibacterial, anti-HIV and anti-malarial activities. On the other hand, polyphenolic compounds, like coumarins and its derivatives are able to bind transition metal ions and inhibit hydroxyl radical and hydrogen peroxide formation produced by Fenton’s reactions. Polyphenol derivatives (or metabolites) were found to have numerous therapeutic applications, such as central nervous system stimulants, antitumor and anti-HIV therapy, antibacterial, anticoagulants etc.
