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Design, synthesis and pharmacological evaluation of hybrid molecules out of quinazolinimines and lipoic acid lead to highly potent and selective butyrylcholinesterase inhibitors with antioxidant properties

Decker, Michael und Kraus, Birgit und Heilmann, Jörg (2008) Design, synthesis and pharmacological evaluation of hybrid molecules out of quinazolinimines and lipoic acid lead to highly potent and selective butyrylcholinesterase inhibitors with antioxidant properties. Bioorganic & medicinal chemistry 16 (8), S. 4252-4261.

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Zusammenfassung

A set of hybrid mols. were synthesized out of lipoic acid, alpha ,w-diamines of different lengths serving as spacers, and cholinesterase (ChE) inhibiting [2,1-b]quinazolinimines. Depending on the length of the alkylene spacer the amide hybrids are inhibitors of acetylcholinesterase (AChE) with inhibitory activities of 0.5-4.6 micro M and inhibitors of butyrylcholinesterase (BChE) with activities ...

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Dokumentenart:Artikel
Datum:2008
Zusätzliche Informationen (Öffentlich):CAN 149:464 1-3 Pharmacology 9000-81-1 (Acetylcholinesterase) Role: BSU (Biological study, unclassified), BIOL (Biological study) (hybrid mols. of quinazolinimines and lipoic acid as butyrylcholinesterase inhibitors with antioxidant properties); 1029034-02-3P; 1029034-03-4P; 1029034-04-5P; 1029034-05-6P; 1029034-06-7P; 1029034-07-8P; 1029034-08-9P; 1029034-09-0P; 1029034-10-3P; 1029034-11-4P; 1029034-12-5P; 1029034-13-6P; 1029034-14-7P; 1029034-15-8P Role: PAC (Pharmacological activity), SPN (Synthetic preparation), THU (Therapeutic use), BIOL (Biological study), PREP (Preparation), USES (Uses) (hybrid mols. of quinazolinimines and lipoic acid as butyrylcholinesterase inhibitors with antioxidant properties); 745837-16-5; 911366-60-4 Role: PAC (Pharmacological activity), THU (Therapeutic use), BIOL (Biological study), USES (Uses) (hybrid mols. of quinazolinimines and lipoic acid as butyrylcholinesterase inhibitors with antioxidant properties); 109-76-2 (1,3-Propanediamine); 110-60-1 (1,4-Butanediamine); 124-09-4 (1,6-Hexanediamine); 373-44-4 (1,8-Octanediamine); 462-94-2 (1,5-Pentanediamine); 646-19-5 (1,7-Heptanediamine); 1200-22-2 (Lipoic acid); 881890-07-9; 911366-48-8 Role: RCT (Reactant), RACT (Reactant or reagent) (hybrid mols. of quinazolinimines and lipoic acid as butyrylcholinesterase inhibitors with antioxidant properties); 9001-08-5 (Butyrylcholinesterase) Role: BSU (Biological study, unclassified), BIOL (Biological study) (inhibitors; hybrid mols. of quinazolinimines and lipoic acid as butyrylcholinesterase inhibitors with antioxidant properties)
Institutionen:Chemie und Pharmazie > Institut für Pharmazie > Lehrstuhl Pharmazeutische Biologie (Prof. Heilmann)
Identifikationsnummer:
WertTyp
2008:495400Andere
Stichwörter / Keywords:Antioxidants Cholinesterase inhibitors Structure-activity relationship (hybrid mols. of quinazolinimines and lipoic acid as butyrylcholinesterase inhibitors with antioxidant properties) butyrylcholinesterase inhibitor antioxidant quinazolinimine lipoate prepn SAR
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
Eingebracht am:18 Okt 2010 13:28
Zuletzt geändert:18 Okt 2010 13:28
Dokumenten-ID:17237
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