Search for: [Abstract = "tionship analysis based on pharmacological screening results. The lead structure for the modifications carried out was \(RS\)\-4\-\[1\-\(2,5\-dichlorophenoxy\)propyl\]\-6\-\(4\-methylpiperazin\-1\-yl\)\-1,3,5\-triazin\-2\-amine \(1.9\), a potent and selective serotonin 5\-HT6 receptor antagonist, synthesized earlier in the Department of Technology and Biotechnology of Drugs JU MC. Forty\-nine final compounds have been obtained, which were divided into series \(A\-E\) containing in the structure, among others\: substitution of the aromatic ring with chlorine and fluorine atoms, a methoxyl group at the triazine ring, substitution of an amino group in the triazine ring, as well as sulfur\-containing compounds. The work plan included rational design using molecular modelling techniques, allowing preliminary evaluation of\: the interaction of compounds with 5\-HT6R, inhibition of selected enzymes, and \"druglikeness\". The designed compounds were obtained via multi\-step synthesis using O\- and S\-alkylation, simple and cyclic condensation as well as Buchwald\-Hartwig reaction. Although no desirable enzyme inhibitors were found, about 30% of the obtained derivatives showed very high affinity towards the 5\-HT6 receptor \(Ki < 20 nM\), including particularly high affinity for seven compounds \(Ki < 10 nM\). A vast majority of the derivatives showed selectivity toward 5\-HT1A and 5\-HT7 receptors. The most active structure wit"]

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