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Structure-Based Search for New Inhibitors of Cholinesterases
Zitieren Sie bitte immer diese URN: urn:nbn:de:bvb:20-opus-129423
- Cholinesterases are important biological targets responsible for regulation of cholinergic transmission, and their inhibitors are used for the treatment of Alzheimer’s disease. To design new cholinesterase inhibitors, of different structure-based design strategies was followed, including the modification of compounds from a previously developed library and a fragment-based design approach. This led to the selection of heterodimeric structures as potential inhibitors. Synthesis and biological evaluation of selected candidates confirmed that theCholinesterases are important biological targets responsible for regulation of cholinergic transmission, and their inhibitors are used for the treatment of Alzheimer’s disease. To design new cholinesterase inhibitors, of different structure-based design strategies was followed, including the modification of compounds from a previously developed library and a fragment-based design approach. This led to the selection of heterodimeric structures as potential inhibitors. Synthesis and biological evaluation of selected candidates confirmed that the designed compounds were acetylcholinesterase inhibitors with \(IC_{50}\) values in the mid-nanomolar to low micromolar range, and some of them were also butyrylcholinesterase inhibitors.…
Autor(en): | Marek Bajda, Anna Wieckowska, Michalina Hebda, Natalia Guzior, Christoph A. Sotriffer, Barbara Malawska |
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URN: | urn:nbn:de:bvb:20-opus-129423 |
Dokumentart: | Artikel / Aufsatz in einer Zeitschrift |
Institute der Universität: | Fakultät für Chemie und Pharmazie / Institut für Pharmazie und Lebensmittelchemie |
Sprache der Veröffentlichung: | Englisch |
Titel des übergeordneten Werkes / der Zeitschrift (Englisch): | International Journal of Molecular Sciences |
Erscheinungsjahr: | 2013 |
Band / Jahrgang: | 14 |
Heft / Ausgabe: | 3 |
Seitenangabe: | 5608-5632 |
Originalveröffentlichung / Quelle: | International Journal of Molecular Sciences 2013, 14, 5608-5632; doi:10.3390/ijms14035608 |
DOI: | https://doi.org/10.3390/ijms14035608 |
Allgemeine fachliche Zuordnung (DDC-Klassifikation): | 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 615 Pharmakologie, Therapeutik |
Freie Schlagwort(e): | acetylcholinesterase; butyrylcholinesterase; cholinesterases inhibitors; drug design; fragment-based design |
Datum der Freischaltung: | 27.06.2016 |
Lizenz (Deutsch): | CC BY: Creative-Commons-Lizenz: Namensnennung |