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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 and Kraus, Birgit and 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), pp. 4252-4261.

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Abstract

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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Item Type:Article
Date:2008
Additional information (public):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)
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann)
Identification Number:
ValueType
2008:495400Other
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
Subjects:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Prof. Dr. Joerg Heilmann
Deposited On:18 Oct 2010 13:28
Last Modified:18 Oct 2010 13:28
Item ID:17237
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