Search for: [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."]

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