Synthetic cannabinoids in drug discovery
Design, synthesis and evaluation of modified coumarins as CB receptor ligands
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The endocannabinoid system represents a highly complex lipid-based (neuro-) transmitter system and can be found in nearly all animals. Since the discovery of the two main cannabinoid receptors CB1 and CB2 in the early '90, intensive research reviled a substantial influence of this system on many physiological and pathophysiological processes. Direct and selective targeting of the system bears a huge potential for the development of novel therapeutic approaches, especially for the treatment of chronical pain, inflammation or other neurological disorders. Therefore, the endocannabinoid system is a promising target in drug development.
In the presented thesis, the design, syntheses and pharmacologic evaluation of substituted coumarins as potential new drug candidates as selective synthetic cannabinoids were investigated. In a combinatorial synthetic approach, several new libraries of new ligands were synthesised and subsequently pharmacological tested.
Additionally, in a second project, novel reversible monoacylglycerol lipase (MAGL) inhibitors have been synthesized and pharmacologically evaluated. Thereby, several important structure-activity relationships for high potency or selectivity were found. Nearly all potencies of the developed inhibitors were determined in the nanomolar regions.
In the presented thesis, the design, syntheses and pharmacologic evaluation of substituted coumarins as potential new drug candidates as selective synthetic cannabinoids were investigated. In a combinatorial synthetic approach, several new libraries of new ligands were synthesised and subsequently pharmacological tested.
Additionally, in a second project, novel reversible monoacylglycerol lipase (MAGL) inhibitors have been synthesized and pharmacologically evaluated. Thereby, several important structure-activity relationships for high potency or selectivity were found. Nearly all potencies of the developed inhibitors were determined in the nanomolar regions.
| Erscheinungsdatum | 26.05.2020 |
|---|---|
| Reihe/Serie | Beiträge zur organischen Synthese ; 88 |
| Sprache | englisch |
| Maße | 145 x 210 mm |
| Einbandart | Paperback |
| Themenwelt | Naturwissenschaften ► Chemie ► Organische Chemie |
| Schlagworte | cannabinoid receptor • drug discovery • GPCR • MAGL • Synthetic cannabinoids |
| ISBN-10 | 3-8325-5103-4 / 3832551034 |
| ISBN-13 | 978-3-8325-5103-2 / 9783832551032 |
| Zustand | Neuware |
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