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Title: Search for the novel GABA and/or monoaminesreuptake inhibitors in the group of 4-hydroxyand4-aminobutanamide derivatives
Abstract:
In this dissertation, a review of the literature data in the field of GABA and monoamine reuptake inhibitors belonging to the solute carrier 6 (SLC6) gene family is presented. Special attention is paid to their potential application in the treatment of neurological disorders such as epilepsy, anxiety, neuropathic pain as well as Parkinson's disease. Considering the interesting results of the previous studies performed at the Department of Medicinal Chemistry JU MC, the aim of the research presented in this PhD dissertation was to design and synthesize new GABA uptake inhibitors, 2-substituted derivatives of the N-benzylamides of 4-hydroxy- and 4-aminobutyric acid and their evaluation toward biological and pharmacological specific targets. According to the aim of the presented research, the chemical modifications of the lead structures had been designed and the library of 129 new compounds belonging to 2-substituted derivatives of 4-hydroxybutanamides and 4-aminobutanamides and their structural analogs had been synthesized. Uptake inhibition toward mGAT1-4 was determined for all the obtained compounds. Additionally, the MS binding assay towards mGAT1, hDAT, hNET and hSERT had been performed. Compounds which displayed interesting profiles in in vitro tests have been subjected to preliminary behavioral studies. The newly synthesized compounds were found to be non-selective GABA re ; uptake inhibitors with various affinities to monoamine reuptake transporters (hDAT, hSERT and hNET). The greatest achievement was the recognition of two potent dopamine transporter inhibitors. In summary, selected compound with outstanding biological and pharmacological properties, can provide an excellent contribution to current knowledge and a promising starting point for the design of new and selective dopamine reuptake inhibitors.
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Last modified:
Jan 24, 2023
In our library since:
Nov 9, 2017
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http://dl.cm-uj.krakow.pl:8080/publication/4206
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| Edition name | Date |
|---|---|
| ZB-126495 | Jan 24, 2023 |
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