Neurodegeneration may occur when the brain is exposed to high level of reactive oxygen species, mitochondrial dysfunction, neurotoxicity, such as excitotoxicity. Administering neuroprotective agents can prevent the chronic conditions damaging nerve cells. Therefore, there is an urgent need to develop effective neuroprotective agents.
The kynurenic acid (KYNA) is capable of interact with the metabolism of neurons and bearing neuroprotective properties. KYNA is a competitive antagonist of NMDA receptors on the neurons. Additionally, KYAN is able to affect the presynaptic release of glutamate via α7 nicotine acetylcholine receptors. Therefore, KYNA is capable to prevent neuron destruction caused by excitotoxic conditions.
According to its polar structure KYNA can penetrate through the blood-brain barrier (BBB) in a very low extent. The present invention solved the functionalization of the C-3 position of KYNA to prepare a compound that is able to penetrate through the BBB and bear effective neuroprotective properties. The C-3 substituted compounds of the invention are able to move through the BBB up to 7 times higher ratio than the currently existing KYNA compounds.
According to its polar structure KYNA can penetrate through the blood-brain barrier (BBB) in a very low extent. The present invention solved the functionalization of the C-3 position of KYNA to prepare a compound that is able to penetrate through the BBB and bear effective neuroprotective properties.
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Top of the Hungarian University education; more than 21000 students, with about 4100 students from foreign countries; the highest level of reseach in Hungary; intellectual property portfolio of 41 patent, 8 know-how; numerous parts of the IP prtfolio is licenced or expoited in spin-off enterprises;
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