SZR-104, a Novel Kynurenic Acid Analogue with High Permeability through the Blood–Brain Barrier

By being an antagonist of glutamate and other receptors, kynurenic acid serves as endogenous neuroprotectant in several pathologies the brain. Unfortunately, systemic administration is hindered by its low permeability through blood–brain barrier. One possibility to overcome this problem use analogues with similar biological activity acid, but increased We synthesized six novel aminoalkylated amide derivatives among which SZR-104 (N-(2-(dimethylamino)ethyl)-3-(morpholinomethyl)-4-hydroxyquinoline-2-carboxamide) proved have highest vitro barrier model. In addition, was significantly higher than that xanthurenic 39B, a quinolone derivative/xanthurenic analogue. Since peripherally administered able inhibit epileptiform brain, we conclude promising analogue good penetrability into central nervous system.