Buch, Englisch, Band 88, 354 Seiten, PB, Format (B × H): 145 mm x 210 mm
Design, synthesis and evaluation of modified coumarins as CB receptor ligands
Buch, Englisch, Band 88, 354 Seiten, PB, Format (B × H): 145 mm x 210 mm
Reihe: Beiträge zur organischen Synthese
ISBN: 978-3-8325-5103-2
Verlag: Logos
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.
Autoren/Hrsg.
Fachgebiete
- Naturwissenschaften Biowissenschaften Chemische Biologie, Synthetische Biologie
- Naturwissenschaften Chemie Physikalische Chemie Chemische Kristallographie
- Naturwissenschaften Chemie Organische Chemie
- Naturwissenschaften Chemie Chemie Allgemein Pharmazeutische Chemie, Medizinische Chemie
- Naturwissenschaften Biowissenschaften Biochemie (nichtmedizinisch)
