3-oxopiperazinium derivatives as agonists of nerve growth factor receptors and their use as medicaments

Abstract

New 3-oxopiperazinium derivatives agonists of Nerve Growth Factor receptors and their use as medicaments. Neurotrophin binding to its specific receptor Trk A leads to the activation of multiple signalling cascades, culminating in neuroregenerative effects, including neuronal survival and neurite outgrowth. Neurotrophic factors have been used for the treatment of several neurodegenerative diseases. However, their use is limited by their inability to cross the blood-brain barrier, their short half life and their side effects. Small molecule neurotrophin peptidomimetics may be beneficial in treating a number of neurodegenerative disorders. The present invention shows the capacity of nerve growth factor agonist molecules derived from the 3- oxopiperazinium scaffold to induce differentiation in PC12 cells and, therefore, that these small molecules with NGF agonist activity may be beneficial for treatment of neurodegenerative diseases, due to their neuroregenerative effects.