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| Dokumentenart: | Artikel | ||||
|---|---|---|---|---|---|
| Titel eines Journals oder einer Zeitschrift: | Journal of medicinal chemistry | ||||
| Verlag: | American Chemical Society | ||||
| Band: | 53 | ||||
| Nummer des Zeitschriftenheftes oder des Kapitels: | 9 | ||||
| Seitenbereich: | S. 3611-3617 | ||||
| Datum: | 2010 | ||||
| Zusätzliche Informationen (Öffentlich): | CAN 152:516583 1-3 Pharmacology 9000-81-1 (Acetylcholinesterase); 9001-08-5 Role: BSU (Biological study, unclassified), BIOL (Biological study) (bivalent beta -carbolines as potential multitarget anti-alzheimer agents); 103800-21-1P; 1225056-56-3P; 1225056-70-1P; 1225056-71-2P; 1225056-72-3P; 1225056-73-4P; 1225056-74-5P; 1225056-75-6P Role: PAC (Pharmacological activity), RCT (Reactant), SPN (Synthetic preparation), THU (Therapeutic use), BIOL (Biological study), PREP (Preparation), USES (Uses), RACT (Reactant or reagent) (bivalent beta -carbolines as potential multitarget anti-alzheimer agents); 244-63-3 (9H-Pyrido[3,4-b]indole); 30684-42-5; 58982-28-8 (9H-Pyrido[3,4-b]indol-6-ol) Role: PAC (Pharmacological activity), RCT (Reactant), THU (Therapeutic use), BIOL (Biological study), USES (Uses), RACT (Reactant or reagent) (bivalent beta -carbolines as potential multitarget anti-alzheimer agents); 5667-11-8P; 53952-75-3P; 950993-91-6P; 1225056-47-2P; 1225056-48-3P; 1225056-49-4P; 1225056-50-7P; 1225056-51-8P; 1225056-52-9P; 1225056-53-0P; 1225056-54-1P; 1225056-55-2P; 1225056-57-4P; 1225056-58-5P; 1225056-59-6P; 1225056-60-9P; 1225056-61-0P; 1225056-62-1P; 1225056-63-2P; 1225056-64-3P; 1225056-65-4P; 1225056-68-7P; 1225056-69-8P; 1225056-76-7P Role: PAC (Pharmacological activity), SPN (Synthetic preparation), THU (Therapeutic use), BIOL (Biological study), PREP (Preparation), USES (Uses) (bivalent beta -carbolines as potential multitarget anti-alzheimer agents); 7212-59-1; 16502-01-5 (1,2,3,4-Tetrahydro-beta -carboline); 20315-68-8 (6-Methoxy-1,2,3,4-Tetrahydro-beta -carboline); 30684-43-6; 59444-69-8 Role: PAC (Pharmacological activity), THU (Therapeutic use), BIOL (Biological study), USES (Uses) (bivalent beta -carbolines as potential multitarget anti-alzheimer agents); 74-88-4 (Methyl iodide); 110-52-1; 110-86-1 (Pyridine); 111-24-0; 112-60-7; 623-24-5; 629-03-8 (1,6-Dibromohexane); 629-27-6; 3344-70-5; 4101-68-2; 4549-31-9; 4549-32-0; 4549-33-1; 16696-65-4; 746549-76-8 Role: RCT (Reactant), RACT (Reactant or reagent) (bivalent beta -carbolines as potential multitarget anti-alzheimer agents); 31255-26-2P; 1225056-66-5P; 1225056-67-6P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (bivalent beta -carbolines as potential multitarget anti-alzheimer agents) | ||||
| Institutionen: | Chemie und Pharmazie > Institut für Pharmazie > Lehrstuhl Pharmazeutische Biologie (Prof. Heilmann) | ||||
| Identifikationsnummer: |
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| Stichwörter / Keywords: | Alzheimer disease Cognitive disorders Enzyme inhibitors NMDA receptor antagonists Neurodegenerative disease Structure-activity relationship (bivalent beta -carbolines as potential multitarget anti-alzheimer agents) NMDA receptors Role: BSU (Biological study, unclassified), BIOL (Biological study) (bivalent beta -carbolines as potential multitarget anti-alzheimer agents) Toxins Role: BSU (Biological study, unclassified), BIOL (Biological study) (excitotoxins bivalent beta -carbolines as potential multitarget anti-alzheimer agents) acetylcholinesterase inhibitor NMDA Alzheimers disease carboline deriv SAR prepn | ||||
| Dewey-Dezimal-Klassifikation: | 500 Naturwissenschaften und Mathematik > 570 Biowissenschaften, Biologie 500 Naturwissenschaften und Mathematik > 540 Chemie | ||||
| Status: | Veröffentlicht | ||||
| Begutachtet: | Ja, diese Version wurde begutachtet | ||||
| An der Universität Regensburg entstanden: | Ja | ||||
| Dokumenten-ID: | 17255 |
Zusammenfassung
Alzheimer's disease (AD) is a prevalent neurodegenerative disorder with multifactorial causes that requires multitargeted treatment. Inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) improve cholinergic signaling in the central nervous system and thus AChE inhibitors are well established in the therapy of AD to improve memory disturbances and other cognitive symptoms. On ...
Zusammenfassung
Alzheimer's disease (AD) is a prevalent neurodegenerative disorder with multifactorial causes that requires multitargeted treatment. Inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) improve cholinergic signaling in the central nervous system and thus AChE inhibitors are well established in the therapy of AD to improve memory disturbances and other cognitive symptoms. On the other hand, AD patients benefit from redn. of pathol. glutamate-induced, Ca2+-mediated excitotoxicity by the N-methyl-D-aspartate receptor (NR) antagonist memantine. New drugs that simultaneously affect both cholinergic transmission and glutamate-induced excitotoxicity may further improve AD treatment. While connecting beta -carboline units by alkylene spacers in two different series of compds. and subsequent evaluation of their AChE/BChE-inhibitory potential, we found that several of these bivalent beta -carbolines were potent NR blockers. The most promising compd. was a N9-homobivalent beta -carboline with a nonylene spacer, which displayed IC50 values of 0.5 nM for AChE, 5.7 nM for BChE, and 1.4 micro M for NR, resp.
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