@misc{Olszak-Płachta_Marta_Pyridinylpiperazine_2022,
 author={Olszak-Płachta, Marta},
 address={Kraków},
 howpublished={online},
 year={2022},
 school={Rada Dyscypliny Nauki farmaceutyczne},
 language={pol},
 abstract={5-HT6 receptors are mainly located in the central nervous system. It has been shown that block-ade of 5-HT6R increases acetylcholine and glutamate level. Acetylcholine and glutamate are neu-rotrasmitters involved in cognitive functions, learning processes, concentrations and memory. The aim of the thesis focuses on synthesis of a new pyridylpiperazine derivatives as a 5-HT6 re-ceptor antagonists that affect central nervous system. Design of compounds based on the four key structural elements for 5-HT6 antagonism: a positive ionizable atom, an aromatic ring, a hy-drogen bond acceptor group, and hydrophobic site. The crucial step of synthesis was Katrizkys Reaction – the formation of the pyridine ring in a one pot process involving the reaction of α,β unsaturated ketones, amines and 1H-benzotriazole-1-acetonitrile. Final free base compounds were converted into HCl or fumaric acid salt. Research allowed to find new very potent and se-lective 5-HT6 receptor antagonist: 1-[4-(4-methoxyphenyl)-6-(oxan-4-ylmethyl)pyridin-2-yl]-4-methylpiperazine (98). This new pyridylpiperazine derivative with very high blood-brain barier permeability, good results for cytochrome P450 inhibition might determine promising strategy for further development in treatment of CNS deseases.},
 title={Pyridinylpiperazine derivatives as 5-HT6 antagonists that affect central nervous system},
 type={Praca doktorska},
 keywords={5-HT 6 R, antagonist, Katritzkis Reaction, pyridinylpiperazine, serotonin},
}